Boronic acid and ester inhibitors of thrombin

ABSTRACT

Novel boronic acid and ester and carboxyl-modified amino acid compounds of the Formula I, which are inhibitors of trypsin-like enzymes, are disclosed:R1-Z-CHR2-A,where R1, Z, R2 arid A are defined within.

This is a division of application Ser. No. 08/364,338, filed Dec. 27, 1994, now U.S. Pat. No. 5,563,127 which is a continuation-in-part of U.S. patent application Ser. No. 8/348/029, filed Dec. 1, 1994, now abandoned, which is a continuation-in-part of U.S. patent application Ser. No. 08/318/029, filed Oct. 4, 1994, now abandoned, which is a continuation-in-part of U.S. patent application Ser. No. 08/036/377, filed Mar. 24, 1993, now abandoned.

FIELD OF THE INVENTION

This invention relates to the discovery of new boronic acid derivatives which are inhibitors of thrombin and pharmaceutical compositions thereof.

BACKGROUND OF THE INVENTION

Hemostasis is the normal physiological process in which bleeding from an injured blood vessel is arrested. It is a dynamic and complex process in which proteolytic enzymes such as thrombin play a key role. Blood coagulation may occur through either of two cascades of zymogen activations, the extrinsic and intrinsic pathways of the coagulation cascade. Factor VIIa in the extrinsic pathway, and Factor IXa in the intrinsic pathway are important determinants of the activation of factor X to factor Xa, which itself catalyzes the activation of prothrombin to thrombin. The last protease in each pathway is thrombin, which acts to hydrolyze four small peptides (two FpA and two FpB) from each molecule of fibrinogen, thus deprotecting its polymerization sites. Once formed, the linear fibrin polymers may be cross-linked by factor XIIIa, which is itself activated by thrombin. In addition, thrombin is a potent activator of platelets, upon which it acts at specific receptors. Thrombin activation of platelets leads to aggregation of the cells and secretion of additional factors that further accelerate the creation of a hemostatic plug. Thrombin also potentiates its own production by the activation of factors V and VIII (see Hemker and Beguin in: Jolles, et. al., "Biology and Pathology of Platelet Vessel Wall Interactions," pp. 219-26 (1986), Crawford and Scrutton in: Bloom and Thomas, "Haemostasis and Thrombosis," pp. 47-77, (1987), Bevers, et. al., Eur. J. Biochem. 1982, 122, 429-36, Mann, Trends Biochemo Sci. 1987, 12, 229-33).

Thrombosis may be regarded as the pathological condition wherein improper activity of the hemostatic mechanism results in intravascular thrombus formation. Etiological factors such as the presence of atherosclerotic plaque, phlebitis and septicemia may cause thrombosis, leading to impaired blood flow to the effected tissues and possible serious pathological consequences. Thrombosis may be reduced by inhibition of the normal process of blood coagulation by anticoagulants. Anticoagulants act by reducing the amount of thrombin which is generated, or by inhibiting with the proteolytic actions of thrombin.

Currently, two of the most effective classes of drugs in clinical use as anticoagulants are the heparins and the vitamin K antagonists. The heparins are ill-defined mixtures of sulfated polysaccharides that bind to, and thus potentiate the action of antithrombin III. Antithrombin III is a naturally occurring inhibitor of the activated clotting factors IXa, Xa, XIa, thrombin and probably XIIa (see Jaques, Pharmacol. Rev. 1980, 31, pp. 99-166). The vitamin K antagonists, of which warfarin is the most well-known example, act indirectly by inhibiting the post-ribosomal carboxylations of the vitamin K dependent coagulation factors II, VII, IX and X (see Hirsch, Semin. Thromb. Hemostasis 1986, 12, 1-11). While effective therapies for the treatment of thrombosis, heparins and vitamin K antagonists have the unfortunate side effects of bleeding and marked interpatient variability, resulting in a small and unpredictable therapeutic safety margin. The use of direct acting thrombin inhibitors is expected to alleviate these problems.

Anticoagulants are also necessary in the processing of blood for therapeutic or diagnostic purposes or for the production of blood products or fragments, since contact of blood with the surfaces commonly used for blood collection and storage causes activation of coagulation leading to thrombin formation and clot formation.

The coagulation proteases thrombin, factor Xa, factor VIIa, and factor IXa are serine proteases having trypsin-like specificity for the cleavage of sequence-specific Arg-Xxx peptide bonds. As with other serine proteases, the cleavage event begins with an attack of the active site serine on the scissile bond of the substrate, resulting in the formation of a tetrahedral intermediate. This is followed by collapse of the tetrahedral intermediate to form an acyl enzyme and release of the amino terminus of the cleaved sequence. Hydrolysis of the acyl enzyme then releases the carboxy terminus.

A number of naturally occurring thrombin inhibitors have been reported. These include nazumamide A from Theonella sp. (see Fusetani, et. al., Tetrahedron Lett. 1991, 32, 707314 4), cyclotheonamide A from Theonella sp. (see Fusetani, et. al., J. Am. Chem. Soc. 1990, 112, 7053-4), amblyommin from Amblyomma hebraeum (see Bonin, et. al., EP 345614), hirudin from Hirudo medicinalis, recombinant versions of hirudin and hirudin fragments (see Rigbl and Jackson, EP 352903, Koerwer, WO 9109946, Meyer, et. al., WO 9108233, Dawson, et. al., WO 9109125, Maraganore, et. al., WO 9102750 and Maraganore, EP 333356).

Synthetic thrombin inhibitors have also been disclosed. Arylsulfonylarginine amides such as (2R,4R)-4-methyl-1- N² -{(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl)sulfonyl}-L-arginyl!-2-piperidinecarboxylate have been shown to be effective inhibitors of thrombin (see Okamoto, et. al. Thromb Res. 1976, 8, 77-82, Ohshiro, et. al., Blood Vessel 1983, 14, 216-8), as have compounds containing constrained arginine mimics such as (2-naphthylsulfonylglycyl)-4-amidino-phenylalanyl piperidide (see Stuerzebecher, et. al., Thromb. Res. 1983, 29, 635-42), 1- 2- 5-(dimethylamino)naphth-1-ylsulfonamido!-3-(2-iminohexahydropyrimidin-5-yl)propanoyl!-4-methylpiperidine dihydrochloride (see Ishikawa, JP 88227572 and Ishikawa and Inamura, JP 88227573), N-(trans-4-amino-methylcyclohexylcarbonyl)-4-O-(2-picolyl)-L-tyrosine 4-acetanilide dihydrochloride (see Okamoto, et. al., EP 217286) and 4- (aminoiminomethyl)amino!benzoic acid esters (see Fuji, et. al., DE 3005580, Matsuoka, et. al., Jpn. J. Pharmacol. 1989, 51, 455-63, and Takeshita, et. al., EP 435235).

Inhibitor design has benefitted from the knowledge of the mechanism of action and of the peptide sequences which are thought to bind in the catalytic site of thrombin, e.g., -Gly-Val-Arg-Gly- of fibrinogen (see Blomback, et. al., J. Biol. Chem., 1972, 247, 1496-512), Ile-Pro-Arg-Ser- of prothrombin (see Magnussen, et. al., in: Reich, et. al., "Proteases and Biological Control," pp. 123-149 (1975)) and -Val-Pro-Arg-Gly- of factor XIII (see Takagi and Doolittle, Biochemistry 1974, 13, 750-6 and Nakamura, et. al., Biochemo Biophys. Res. Commun. 1974, 58, 250-256). This class of mechanism-based inhibitors are exemplified by the tripepride aldehyde D-Phe-Pro-N-Me-Arg-H (see Bajusz, et. al., J. Med. Chem. 1990, 33, 1729-35), the chloromethyl ketone Ac-D-Phe-Pro-ArgCH₂ Cl (see Kettner and Shaw, Thromb. Res. 1979, 14, 969-73) and the trifluoromethyl ketone D-Phe-Pro-ArgCF₃ (see Kolb, et. al., U.S. Pat. No. 697,987).

Kettner and Shenvi (EP 293881, published Jun. 12, 1988), disclose peptide boronic acid inhibitors of trypsin-like proteases of formula (1)

    R.sup.1 - (A.sup.3).sub.q (A.sup.2).sub.p (A.sup.1).sub.o !.sub.n -NH-CHR.sup.2 -BY.sup.1 Y.sup.2                           ( 1)

wherein Y¹ and Y², independently, are hydroxyl or fluoro or, taken together, form a moiety derived from a dihydroxy compound having at least two hydroxy groups separated by at least two connecting atoms in a chain or ring, said chain or ring comprising 1 to about 20 carbon atoms and, optionally, a heteroatom which can be N, S, or O; R² is a substituted alkyl selected from the group consisting of --(CH₂)_(z) --X, --(CH(CH₃)--(CH₂)₂ --X, --CH₂ --CH--(CH₃)--CH₂ --X, --(CH₂)₂ --CH (CH₃)--X and --(CH₂)₂ --CH(CH₃)₂ --X, where X is --NH₂, --NH--C(NH)--NH₂ or --S--C(NH)--NH₂, and z is 3 to 5; n, o, p and q are, independently, either 0 or 1; A¹, A² and A³ are, independently, amino acids of L- or D-configuration selected from the group consisting of Ala, Arg, Asn, Asp, Cys, Gln, Glu, Gly, His, Ile, Leu, Lys, Met, Phe, Pro, Ser, Thr, Trp, Tyr and Val; and R¹ is a peptide comprised of 1 to about 20 amino acids, an acyl or a sulfonyl group comprised of 1 to about 20 carbon atoms, H, or an N-terminal protecting group. In this disclosure, Kettner and Shenvi demonstrated that the pinanediol esters of boropeptides are pharmacogolically equivalent to the corresponding boronic acids. Metternich (EP 0471651 A2) discloses borolysine thrombin inhibitors of formula (2)

    W-Y-NR.sup.4 -CHR.sup.5 -BQ.sup.1 Q.sup.2                  ( 2)

wherein W is an N-protecting group; Y is a sequence of n amino acids such that the n+1 amino acid peptide Y-Lys or Y-Arg has an affinity for the active site of a trypsin-like protease; where n is an integer of from 1 to 10 and in which at least one amino acid is an unnatural amino acid having a hydrophobic side chain; Q¹ and Q² are the same or different and are selected from --OH, --COR₁, --CONR₁ R₂, --NR₁ R₂ or --OR₃ of Q¹ and Q² taken together form a diol residue; R₁, R₂ and R₃ which may be the same or different, are C₁₋₁₀ alkyl, C₆₋₁₀ aryl, C₆₋₁₀ aralkyl, or phenyl substituted by up to three groups selected from C₁₋₄ alkyl, halogen and C₁₋₄ alkoxy; R₄ is hydrogen or C₁₋₁₀ alkyl; R₅ is a group --A--X; wherein A is --(CH₂)_(z) -- in which z is 2, 3, 4 or 5; --CH(CH₃)--(CH₂)₂ --; --CH₂ --CH(CH₃)--CH₂ --; --(CH₂)₂ --CH(CH₃)--; --(CH₂)₂ --C(CH₃)₂ --; CH(CH₃)--(CH₂)₃ --; --CH₂ --CH(CH₃)--(CH₂)₂ --; --CH₂ --CH₂ --CH(CH₃)--CH₂ --; --(CH₂)₃ --CH(CH₃)--; --(CH₂)₃ --C(CH₃)₂ : C₆₋₁₀ aryl C₆₋₁₀ aralkyl and X is --NH₂, --NH--C(NH)--NH₂, --S--C(NH)--NH₂, N₃, -C₁₋₄ alkoxy, C₁₋₄ alkylthio or Si(CH₃)₃ or R₄ and R₅ taken together form a trimethylene group and the asymmetric carbon atom may have the D- or L-configuration or represent any mixture of these.

Surprising for their lack of a basic residue at P₁ are tripeptide thrombin inhibitors comprised of 1-aminoboronic and 1-aminophosphonic acid analogs of 3-methoxy-propylglycine (see Claeson, et. al., U.S. Ser. No. 07-245428) and pentylglycine (see Cheng, et. al., "Symposium on Thrombosis and Hemostasis," 1991, Amsterdam, Abstract 2150).

In addition to thrombin inhibition, boropeptides have been disclosed with utility as a treatment for tumors, viral infections and arthritis (U.S. Pat. No. 4,963,655 and EP 354522A), emphysema (U.S. Pat. No. 4,499,082), hypertension (EP 315574A) and as factor VII/VIIa inhibitors (WO 8909612A). Kleemann, et. al. (AU A-24693/88) disclose renin-inhibiting 1-amino boronic acid derivatives of formula (3)

    A.sup.1 --A.sup.2 --HN--CHR.sup.2 --BXR.sup.3 (YR.sup.4)   (3)

in which A¹ denotes a radical of formulae (4-8).

    R.sup.1 NR.sup.6 --CHR.sup.5 --C═O--                   (4)

    R.sup.1 CHR.sup.12 --CHR.sup.5 --C═O--                 (5)

    R.sup.1 NR.sup.6 --CHR.sup.5 --CHR.sup.7 --CHR.sup.8 --CHR.sup.9 --C═O--(6)

    R.sup.1 CHR.sup.12 --CHR.sup.5 --CHR.sup.7 --CHR.sup.8 --CHR.sup.9 --C═O--                                               (7)

    R.sup.10 --(CH.sub.2).sub.n --CH(CH.sub.2).sub.m R.sup.11 --C═O--(8)

Despite the foregoing, more efficacious and specific inhibitors of coagulation proteases are needed as potentially valuable therapeutic agents for the treatment of thrombosis. None of the cited references describe or suggest the new thrombin-inhibiting boronic acid derivatives of the present invention.

SUMMARY OF THE INVENTION

This invention pertains to novel compounds of formula (I):

    R.sup.1 --Z--CHR.sup.2 --A                                 (I)

wherein

A is

a) --BY¹ Y²,

b) --C(═O)CF₃,

c) --C(═O)CHF₂,

d) --C(═O)CH₂ F,

e) --C(═O)CH₂ Cl,

f) --C(═O)OR³,

g) --C(═O)NR¹⁵ R¹⁶,

h) --C(═O)R³,

i) --C(═O)COOR³,

j) --C(═O)C(═O)NR¹⁵ R¹⁶,

k) --C(═O)C(═O)R³,

l) --C(═O)CY³ Y⁴ COOR³,

m) --C(═O)CY³ Y⁴ C(═O)NR¹⁵ R¹⁶,

n) --C(═O)CY³ Y⁴ C(═O)R³,

o) --PO₃ H₂, or

p) --CHO;

Y¹ and Y² are independently

a) --OH,

b) --F,

c) --NR³ R⁴, or

d) C₁ -C₈ alkoxy;

Y¹ and Y² can be taken together to form:

e) a cyclic boron ester where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which can be N, S, or O,

f) a cyclic boron amide where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which can be N, S, or O,

g) a cyclic boron amide-ester where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which can be N, S, or O;

Y³ and Y⁴ are independently

a) --OH or

b) --F;

Z is

a) --(CH₂)_(m) CONR⁸ --,

b) --(CH₂)_(m) CSNR⁸ --,

c) --(CH₂)_(m) SO₂ NR⁸ --,

d) --(CH₂)_(m) CO₂ --,

e) --(CH₂)_(m) C(S)O--, or

f) --(CH₂)_(m) SO₂ O--;

R¹ is

a) --(CH₂)_(p) -aryl, wherein aryl is phenyl, naphthyl or biphenyl substituted with one, two or three substituents selected from the group consisting of:

halo (F, Cl, Br, I), methylenedioxy, --R⁸, --NR⁸ COR⁹, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, --(CH₂)_(w) --OR⁸, -(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, --(CH₂)_(w) CF₃, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CHO; --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹. --(CH₂)_(w) SO₂ NH--(C₁ -C₅)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN⁴ H, --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl ), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO₂ --(phenyl), --O(C═O)--(C₁ -C₅ -alkyl), ##STR1## b) heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted:

quinolinyl,

ii) isoquinolinyl,

iii) benzopyranyl,

iv) benzothiophenyl,

v) benzofuranyl,

vi) 5,6,7,8-tetrahydroquinolinyl,

vii) 5,6,7,8-tetrahydroisoquinolinyl,

and wherein the substituents are selected from the group consisting of halo (F, Cl, Br, I), --CN, C₁ -C₁₀ -alkyl, C₃ -C₈ -cycloalkyl, C₂ -C₁₀ -alkenyl, C₂ -C₁₀ -alkynyl, R⁸, --OR⁸, --NO₂, --CF₃, --S(O)_(r) R⁷, --NR⁸ R⁹, --COR⁸, --CO₂ R⁸, --CONHR⁸, NR⁸ COR⁹, NR⁸ CO₂ R⁹, ##STR2## wherein J is N or C and K, L, M and Q are independently selected at each occurrence from the group consisting of N, CR¹³, S or O, provided that:

i) there may be only one S or O present in the ring at a time;

ii) there may only be 1-2N present when there is an O or S present;

iii) there may be only 1-4N present;

g) ##STR3## wherein W, R, T, U and V are selected from the group consisting of: CR¹³ or N, provided that there be no less than 1 and no more than 3N present; ##STR4## is as defined above; ##STR5## is as defined above; ##STR6## wherein G is O, S, or NP, where P is an amine protecting group selected from the group consisting of: --R³, --C(═O)R³, --SO₂ R³, --C(═O)OR³); ##STR7## wherein G is O, S, or NP, where P is an amine protecting group selected from the group consisting of: --R³, --C(═O)R³, --SO₂ R³, --C(═O)OR³);

R² is

a) --(C₁ -C₁₂ alkyl)--X,

b) --(C₂ -C₁₂ alkenyl)--X, or ##STR8## X is a) halogen (F, Cl, Br, I),

b) --CN,

c) --NO₂,

d) --CF₃,

e) --S(O)_(r) R¹⁴,

f) --NHR¹⁴

g) --NHS(O)_(r) R¹⁴,

h) --NHC(NH)H,

i) --NHC(NH)NHOH,

j) --NHC(NH)NSCN,

k) --NHC(NH)NHR¹⁴,

l) --NHC(NH)NHCOR¹⁴,

m) --C(NH)NHR¹⁴,

n) --C(NH)NHCOR¹⁴,

o) --C(O)NHR¹⁴,

p) --C(O)NHC(O)R¹⁴,

q) --C(O)OR¹⁴,

r) --OR¹⁴,

s) --OC(O)R¹⁴,

t) --OC(O)OR¹⁴,

u) --OC(O)NHR¹⁴,

v) --OC(O)NHC(O)R¹⁴,

w) --SC(═NH)NHR¹⁴, or

x) --SC(═NH)NHC(═O)R¹⁴ ;

R³ is

a) hydrogen,

b) C₁ -C₈ alkyl,

c) --(C₁ -C₄ alkyl)-aryl,

d) C₅ -C₇ cycloalkyl,

e) phenyl; or

R⁴ is

a) hydrogen,

b) C₁ -C₈ alkyl,

c) -(C₁ -C₄ alkyl)-aryl,

d) C₅ -C₇ cycloalkyl,

e) phenyl, or

f) phenylsulfonyl;

R⁵ and R⁶ are hydrogen or when taken together form a six membered aromatic ring optionally substituted with one, two or three substituents selected from the group consisting of halo (F, Cl, Br, I), --CN, C₁ -C₁₀ -alkyl, C₃ -C₈ -cycloalkyl, C₂ -C₁₀ -alkenyl, C₂ -C₁₀ -alkynyl, --OR⁸, --NO₂, --CF₃, --S(O)_(r) R⁷, --NR⁸ R⁹, --COR⁸, --CO₂ R⁸, --CONR⁸ R⁹, phenyl, benzyl, phenylethyl;

R⁷ is

a) phenyl,

b) C₁ -C₈ -alkyl,

c) C₁ -C₄ -alkoxy,

d) --CF₃, or

e) benzyl;

R⁸ and R⁹ are independently

a) H, ##STR9## c) C₃ -C₇ cycloalkyl, or d) C₁ -C₈ -alkyl;

R¹¹ is

a) halo (F, Cl, Br, I),

b) --CN,

c) C₁ -C₁₀ -alkyl,

d) C₃ -C₈ -cycloalkyl,

e) C₂ -C₁₀ -alkenyl,

f) C₂ -C₁₀ -alkynyl,

g) --OR⁸,

h) --NO₂,

i) --CF₃,

j) --S(O)_(r) R⁷,

k) --NR⁸ R⁹,

l) --COR⁹,

m) --CO₂ R⁸,

n) --CONR⁸ R⁹, or

o) H

R¹² is

H, C₁ -C₄ alkyl, phenyl, benzyl, --COR⁷, or --S(O)_(r) R⁷ ;

R¹³ is

H, halogen (F, Cl, Br, I), (C₁ -C₈)alkyl, (C₁ -C₆)-perfluoroalkyl, --(CH₂)_(r) --D, C₃ -C₈ cycloalkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, methylenedioxy, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) NC, --(CH₂)_(w) CN, --(CH₂)_(w) NO₂, --(CH₂)_(w) CF₃, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) SO₂ NH--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN⁴ H, --O(C═O)--(C₁ -C₅ -alkyl), --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO₂ --(phenyl), --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸, --S--(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸, or --O--(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸ ;

R¹⁴ is

a) --H,

b) --CF₃

c) -C₁ -C₄ alkyl,

d) --(CH₂)_(q) -aryl, wherein aryl is phenyl, biphenyl, naphthyl, or fluorenyl unsubstituted or substituted with one to three substituents selected from the group consisting of:

halogen (F, Cl, Br, I),

--CF₃,

-(C₁ -C₄ alkyl),

--(CH₂)_(x) R¹⁵,

--(CH₂)_(x) CO(CH₂)_(y) R¹⁵,

--(CH₂)_(x) C(O)O(CH₂)_(y) R¹⁵,

--(CH₂)_(x) C(O)N (CH₂)_(y) R¹⁵ ! (CH₂)_(y) R¹⁶ !,

-methylenedioxy,

--(C₁ -C₄ alkoxy),

--(CH₂)_(x) O(CH₂)_(y) R¹⁵,

--(CH₂)_(x) OCO(CH₂)_(y) R¹⁵,

--(CH₂)_(x) OC(O)O(CH₂)_(y) R¹⁵,

--(CH₂)_(x) OC(O)N (CH₂)_(y) R¹⁵ ! (CH₂)_(y) R¹⁶ !,

--(CH₂)_(x) OC(O)N (CH₂)_(y) R¹⁵ ! CO(CH₂)_(y) R¹⁶ !,

--(CH₂)_(x) S(O)_(r) (CH₂)_(y) R¹⁵,

--(CH₂)_(x) S(O)_(r) (CH₂)_(y) COR¹⁵,

--(CH₂)_(x) S(O)_(r) (CH₂)_(y) C(O)OR¹⁵,

--(CH₂)_(x) S(O)_(r) N (CH₂)_(y) R¹⁵ ! (CH₂)_(y) R¹⁶ !

--(CH₂)_(x) N (CH₂)_(y) R¹⁵ ! (CH₂)_(y) R¹⁶ !,

--(CH₂)_(x) N (CH₂)_(y) R¹⁵ ! CO(CH₂)_(y) R¹⁶ !,

--(CH₂)_(x) N (CH₂)_(y) R¹⁵ ! C(O)O(CH₂)_(y) R¹⁶ !,

--(CH₂)_(x) N (CH₂)_(y) R¹⁵ !CON (CH₂)_(y) R¹⁵ ! (CH₂)_(y) R¹⁶ !,

--(CH₂)_(x) N (CH₂)_(y) R¹⁵ !CON (CH₂)_(y) R¹⁵ !-- CO(CH₂)_(y) R¹⁶ !,

--(CH₂)_(x) N (CH₂)_(y) R¹⁵ ! S(O)_(r) (CH₂)_(y) R¹⁶ !;

R¹⁵ and R¹⁶ are independently

a) hydrogen,

b) C₁ -C₈ alkyl,

c) -(C₁ -C₄ alkyl)-aryl, where aryl is defined above,

d) C₅ -C₇ cycloalkyl,

e) phenyl, substituted by 0-3 R¹⁸,

f) benzyl, substituted by 0-3 R¹⁸, or

g) -(C₁ -C₄ alkoxy);

R¹⁵ and R¹⁶ can be taken together to form a ring: ##STR10## R¹⁸ and R¹⁹ are independently H, halo (F, Cl, Br, I), C₁ -C₈ -alkyl, C₃ -C₈ cycloalkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, --(CH₂)_(w) CF₃, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) ^(CONR) ⁸ R9, --(CH₂)_(w) SO₂ NH--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN⁴ ^(H), --O(C═O)--(C₁ -C₅ -alkyl), --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -phenyl), or --O(C═O)phenyl;

R¹⁸ and R¹⁹ can be taken together to form a methylenedioxy group;

R²⁰ and R^(20a) are independently (C₁ -C₈)alkyl, --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸, (C₁ -C₆)-perfluoroalkyl, or --(CH₂)_(r) --D;

m is 0 to 6;

n is 1 to 2;

p is 0 to 2;

q is 0 to 4.

r is 0 to 2;

s is 0 to 3;

t is 1 to 5;

u is 0 to 5;

v is 0 to 5;

w is 0 to 5;

x is 0 to 6;

y is 0 to 6;

D is fur-2-yl, fur-3-yl, thiophen-2-yl, thiophen-3-yl, oxazol-2-yl, oxazol-4-yl, thiazol-2-yl, thiazol-4-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, pyrid-2-yl, pyrid-4-yl, pyridazin-3-yl, pyridazin-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrazin-2-yl, or tetrazolyl;

E is --CO--, --SO₂ --, --CH₂ -- or a single bond;

F is --CO--;

W is

a) --O--,

b) --S(O)_(r) --,

c) --NR⁴ --,

d) --NC(═O) R³ --,

e) a bond, or

f) --(CH₂)_(n) --;

or prodrugs or pharmaceutically acceptable salts thereof.

Preferred compounds of formula (I) are those compounds wherein:

Z is

a) --(CH₂)_(m) CONR⁸ --,

b) --(CH₂)_(m) CSNR⁸ --,

c) --(CH₂)_(m) SO₂ NR⁸ --,

R¹ is

a) --(CH₂)_(p) -aryl, wherein aryl is phenyl, naphthyl or biphenyl substituted with one, two or three substituents selected from the group consisting of:

halo (F, Cl, Br, I), methylenedioxy, --R⁸, --NR⁸ COR⁹, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, --(CH₂)_(w) --OR⁸, -(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, --(CH₂)_(w) CF₃, --(CH₂)_(w) S (O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹. --(CH₂)_(w) SO₂ NH--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN⁴ H, e--O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -perfluoroalkyl), or --(CH₂)_(w) NH--CO₂ --(phenyl), --O(C═O--(C₁ -C₅ alkyl);

b) heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted:

i) quinolinyl,

ii) isoquinolinyl,

iii) benzopyranyl,

iv) benzothiophenyl,

v) benzofuranyl,

vi) 5,6,7,8-tetrahydroquinolinyl,

vii) 5,6,7,8-tetrahydroisoquinolinyl,

and wherein the substituents are selected from the group consisting of halo (F, Cl, Br, I), --CN, C₁ -C₁₀ -alkyl, C₃ -C₈ -cycloalkyl, C₂ -C₁₀ -alkenyl, C₂ -C₁₀ -alkynyl, R⁸, --OR⁸, --NO₂, --CF₃, --S(O)_(r) R⁷, --NR⁸ R⁹, --COR⁸, --CO₂ R⁸, --CONR⁸ H, NR⁸ COR⁹, NR⁸ CO₂ R⁹ ; ##STR11## f) wherein the ring ##STR12## represented by --J--K--L--M--Q-- is a group selected from: 1) --N--C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--,

2) --N--C(R¹³)═C(R¹³)--C(R¹³)═N--,

3) --N--C(R¹³)═C(R¹³)--N═C(R¹³)--,

4) --N--C(R¹³)═N--C(R¹³)═N--,

5) --N--C(R¹³)═C(R¹³)--N═N--

6) --N--C(R¹³)═N--N═N--,

7) --N--N═C(R¹³)--N═N--,

8) ═C--0--C(R¹³)═N--C(R¹³)═,

9) --C═C(R¹³)--O--C(R¹³)═N--,

10) ═C--O--C(R¹³)═C(R¹³)--N═,

11) --C═C(R¹³)--C(R¹³)═N--O--,

12) ═C--C(R¹³)═C(R¹³)--O--N═,

13) --C═C(R¹³)--O--N═C(R¹³)--,

14) ═C--S--C(R¹³)═N--C(R¹³)═,

15) --C═C(R¹³)--S--C(R¹³)═N--,

16) ═C--S--C(R¹³)═C(R¹³)--N═,

17) --C═N--S--N═C(R¹³)--,

18) --C═N--S--C(R¹³)═N--,

19) ═C--S--N═C(R¹³)--N═,

20) ═C--S--C(R¹³)═C(R¹³)--C(R¹³)═,

21) --C═C(R¹³)--S--C(R¹³)═C(R¹³)--,

22) ═C--O--C(R¹³)═C(R¹³)--C(R¹³)═, or

23) --C═C(R¹³)--O--C(R¹³)═C(R¹³)--;

g) wherein the ring ##STR13## represented by --C--W--R--T--U--V-- is a group selected from: 1) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--,

2) --C═C(R¹³)--N═C(R¹³)--C(R¹³)═C(R¹³)--,

3) --C═C(R¹³)--C(R¹³)═N--C(R¹³)═C(R¹³)--,

4) --C═N--N═C(R¹³)--C(R¹³)═C(R¹³)--,

5) --C═C(R¹³)--N═N--C(R¹³)═C(R¹³)--,

6) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═N--,

7) --C═N--C(R¹³)═C(R¹³)--N═C(R¹³)--,

8) --C═N--C(R¹³)═N--C(R¹³)--N═C(R¹³)--,

9) --C═C(R¹³)--N═C(R¹³)--N═C(R¹³)--,

10) --C═N--C(R¹³)═N--N═C(R¹³)--,

11) --C═N--C(R¹³)═C(R¹³)--N═N--, or

12) --C═C(R¹³)--N═C(R¹³)--N═N--; ##STR14## is as defined above; ##STR15## is as defined above; ##STR16## wherein G is O, S, or NP (where P is an amine protecting group selected from the group consisting of: --R³, --C(═O)R³, --SO₂ R³, --C(═O)OR³ ; ##STR17## wherein G is O, S, or NP (where P is an amine protecting group selected from the group consisting of: --R³, --C(═O)R³, --SO₂ R³, --C(═O)OR³ ;

R¹⁴ is

a) --H,

b) --CF₃

c) -C₁ -C₄ alkyl,

d) --(CH₂)_(q) -aryl, wherein aryl is phenyl, biphenyl, naphthyl, or fluorenyl unsubstituted substituted with one to three substituents selected from the group consisting of:

halogen (F, Cl, Br, I),

--CF₃,

-(C₁ -C₄ alkyl),

-methylenedioxy,

-(C₁ -C₄ alkoxy),

--(CH₂)_(x) N (CH₂)_(y) R¹⁵ ! (CH₂)_(y) R¹⁶ !; and all other required substituents of formula (I) are as defined in Claim 1.

More preferred compounds of the formula (I) are those compounds wherein:

A is

a) --BY¹ Y²,

b) --C(═O)CF₃,

c) --C(═O)CHF₂,

d) --C(═O)CH₂ F,

e) --C(═O)CH₂ Cl,

f) --C(═O)R³,

g) --C(═O)NR¹⁵ R¹⁶,

h) --C(═O)R³,

i) --C(═O)COOR³,

j) --C(═O)C(═O)NR¹⁵ R¹⁶,

k) --C(═O)C(═O)R³ ,

l) --CHO;

Y¹ and Y² are independently

a) --OH, or

b) C₁ -C₈ alkoxy;

Y¹ and Y² can be taken together to form a cyclic boron ester where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which can be N, S, or O,

Z is

a) --(CH₂)_(m) CONR⁸ --,

b) --(CH₂)_(m) CSNR⁸ --, or

c) --(CH₂)_(m) SO₂ NR⁸ --;

R¹ is

a)--(CH₂)_(p) -aryl, wherein aryl is phenyl, naphthyl or biphenyl substituted with one, two or three substituents independently selected at each occurrence from the group consisting of:

halo (F, Cl, Br, I), methylenedioxy, --R⁸, --NR⁸ COR⁹, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, --(CH₂)_(w) --OR⁸, --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO², --(CH₂)_(w) CF₃, --(CH₂)_(w) S (O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) SO₂ NH--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN⁴ H, --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -perfluoroalkyl), or --(CH₂)_(w) NH--CO₂ --(phenyl), --O(C═O)--C₁ -C₅ -alkyl);

b) heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted:

i) quinolinyl,

ii) isoquinolinyl,

iii) benzopyranyl,

iv) benzothiophenyl,

v) benzofuranyl,

vi) 5,6,7,8-tetrahydroquinolinyl,

vii) 5,6,7,8-tetrahydroisoquinolinyl,

wherein the substituents are members selected from the group consisting of: halo (F, Cl, Br, I), --CN, C₁ -C₁₀ -alkyl, C₃ -C₈ -cycloalkyl, C₂ -C₁₀ -alkenyl, C₂ -C₁₀ -alkynyl, R⁸, --OR⁸, --NO₂, --CF₃, --S(O)_(r) R⁷, --NR⁸ R⁹, --COR⁸, --CO₂ R⁸, --CONR⁸ H, NR⁸ COR⁹, NR⁸ CO₂ R⁹ ; ##STR18## wherein the ring represented by --J--K--L--M--Q-- is a group selected from:

1) --N--C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--,

2) --N--C(R¹³)═C(R¹³)--C(R¹³)═N--,

3) --N--C(R¹³)═C(R¹³)--N═C(R¹³)--,

4) --N--C(R¹³)═N--C(R¹³)═N--,

5) --N--C(R¹³)═C(R¹³)--N═N--

6) --N--C(R¹³)═N--N═N--,

7) --N--N═C(R¹³)--N═N--,

8) ═C--O--C(R¹³)═N--C(R¹³)═,

9) --C═C(R¹³)O--C(R¹³)═N--,

10) ═C--C(R¹³)═C(R¹³)--N═,

11) --C═C(R¹³)--C(R¹³)═N--O--,

12) ═C═C(R¹³)═C(R¹³)--O--N═,

13) --C═C(R¹³)--O--N═C(R¹³)--,

14) ═C--S--C(R¹³)═N--C(R¹³)═,

15) --C═C(R¹³)--S--C(R¹³)═N--,

16) ═C--S--C(R¹³)═C(R¹³)--N═,

17) ═C--S--C(R¹³)═C(R¹³)--C(R¹³)═,

18) --C═C(R¹³) --S--C(R¹³)═C(R¹³)--,

19)═C--O--C(R¹³)═C(R¹³)--C(R¹³)═, or

20)--C═C(R¹³)--O--C(R¹³)═C(R¹³)--; ##STR19## wherein the ring represented by --C--W--R--T--U--V-- is a group selected from:

1)--C═N--C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--,

2)--C═C(R¹³)--N═C(R¹³)--C(R¹³)═C(R¹³)--,

3)--C═C(R¹³)--C(R¹³)═N--C(R¹³)═C(R¹³)--,

4)--C═N--N═C(R¹³)--C(R¹³)═C(R¹³)--,

5)--C═C(R¹³)--N═N--C(R¹³)═C(R¹³)--,

6)--C═N--C(R¹³)═C(R¹³)--C(R¹³)═N--

7)--C═N--C(R¹³)═C(R¹³)--N═C(R13)--,

8)--C═N--C(R¹³)═N--C(R¹³)═C(R¹³)--,

9)--C═C(R¹³)--N═C(R¹³)--N═C(R13)--,

10)--C═N--C(R¹³)═N--N═C(R¹³)--,

11)--C═N--C(R¹³)═C(R¹³)--N═N--, or

12)--C═C(R¹³)--N═C(R¹³)--N═N--; ##STR20## is as defined above; ##STR21## is as defined above; or ##STR22## wherein G is O, S, or NP (where P is an amine protecting group selected from the group consisting of: --R³, --C(═O)R³, --SO₂ R³, --C(═O)OR³);

R² is

a) -(C₁ -C₁₂ alkyl)--X,

b) -(C₂ -C₁₂ alkenyl)--X, or ##STR23## X is a) halogen (F, Cl, Br, I),

b) --CN,

c) --NO₂,

d) --CF₃,

e) --NHR¹⁴

f) --NHS(O)_(r) R¹⁴,

g) --NHC(NH)H,

h) --NHC(NH)NHOH,

i) --NHC(NH)NHCN,

j) --NHC(NH)NHR¹⁴,

k) --NHC(NH)NHCOR¹⁴,

l) --C(NH)NHR¹⁴,

m) --C(NH)NHCOR¹⁴,

n) --C(O)NHR¹⁴,

o) --C(O)NHC(O)R¹⁴,

p) --C(O)OR¹⁴,

q) --OR¹⁴

r) --OC(O)R¹⁴,

s) --OC(O)OR¹⁴,

t) --OC(O)NHR¹⁴,

u) --OC(O)NHC(O) R¹⁴,

v) --SC(═NH)NHR¹⁴, or

w) --SC(═NH)NHC(═O) R¹⁴ ;

R¹³ is

H, halogen (F, Cl, Br, I), (C₁ -C₆) alkyl, --(CH₂)_(r) --D, methylenedioxy, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) NC, --(CH₂)_(w) CN, --(CH₂)_(w) NO², --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) SO₂ NH--(C₁ -C₅)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ --phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN⁴ H, --O(C═O)--(C₁ -C₅ -alkyl), --O(CH₂)_(w) CN, --NH (CH₂)_(w) CN, --S (CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -phenyl), --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸, or --O(C═O)phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸ ;

R¹⁴ is

a) --H,

b) --CF₃

c) -C₁ -C₄ alkyl,

d) --(CH₂)_(q) -aryl, wherein aryl is phenyl, biphenyl, naphthyl, or fluorenyl are optionally substituted with one to three substituents selected from the group consisting of:

halogen (F, Cl, Br, I),

--CF₃,

-(C₁ -C₄ alkyl),

-methylenedioxy,

-(C₁ -C₄ alkoxy), or

--CH₂)_(x) N (CH₂)_(y) R¹⁵ ! CH₂)_(y) R¹⁶ !;

R¹⁸ and R¹⁹ are independently

H, halo (F, Cl, Br, I, C₁ -C₆ -alkyl, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) CN, --(CH₂ WCN, --(CH₂)_(w) NO₂, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) SO₂ NH--(C₁ -C₅)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN⁴ H, --O(C═O)--(C₁ -C₅ -alkyl), --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -phenyl), --(CH₂)_(w) NH--CO₂ (C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -phenyl), or --O(C═O)phenyl;

R¹⁸ and R¹⁹ can be taken together to form a methylenedioxy group;

R²⁰ and R^(20a) are independently (C₁ -C₈)alkyl, --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸, (C₁ -C₆)-perfluoroalkyl, or --(CH₂)_(r) --D;

D is fur-2-yl, fur-3-yl, thiophen-2-yl, thiophen-3-yl, oxazol-2-yl, oxazol-4-yl, thiazol-2-yl, thiazol-4-yl, pyrid-2-yl, pyrid-4-yl, pyrimidin-2-yl, or pyrimidin-4-yl;

W is

a) --O--,

b) --NR⁴ --,

c) a bond, or

d) --(CH₂)_(n) --;

and all other required substituents of formula (I) are as defined in Claim 2.

Most preferred compounds of the formula (I) are those compounds wherein:

A is --BY¹ Y² ;

Y¹ and Y² are --OH;

Y¹ and Y² can be taken together to form a cyclic boron ester where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which can be N, S, or O,

Z is --(CH₂)_(m) CONR⁸ --;

R¹ is

a) --(CH₂)_(p) -aryl, wherein aryl is phenyl, naphthyl or biphenyl substituted with one, two or three substituents selected from the group consisting of:

halo (F, Cl, Br, I), methylenedioxy, --R⁸,--NR⁸ COR⁹, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, --(CH₂)_(w) --OR⁸, --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, --(CH₂)_(w) CF₃, --(CH₂)_(w) S (O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, (CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹. --(CH₂)_(w) SO₂ NH--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN⁴ H, --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -perfluoroalkyl), or --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -phenyl);

b) heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted isoquinolinyl wherein the substituents are members selected from the group consisting of:

halo (F, Cl, Br, I), --CN, C₁ -C₁₀ -alkyl, C₃ -C₈ -cycloalkyl, C₂ -C₁₀ -alkenyl, C₂ -C₁₀ -alkynyl, R⁸, --OR⁸, --NO₂, --CF₃, --S(O)_(r) R⁷, --NR⁸ R⁹, --COR⁸, --CO₂ R⁸, --CONR⁸ R⁹, NR⁸ COR⁹, NR⁸ CO₂ R⁹, ##STR24## wherein the ring represented by --J--K--L--M--Q-- is a group selected from:

1) --N--C(R¹³)═N--C(R¹³)═N--,

2) --N--C(R¹³)═C(R¹³)--N═N--,

3) --N--N═C(R¹³)--N═N--,

5) --N--C(R¹³)═N--N═N--,

6) ═C--S--C(R¹³)═C(R¹³)--C(R¹³)═, or

7) ═C--O--C(R¹³)═C(R¹³)--C(R¹³)═; ##STR25## wherein the ring represented by --C--W--R--T--U--V-- is a group selected from:

1) --C═N--C(R¹³)═C(R¹³)═C(R¹³)--C(R13)═C(R.sup.13)--,

1) --C═C(R¹³)--N═C(R¹³)--C(R¹³)═C(R¹³)--,

2) --C═C(R¹³)--C(R¹³)═N--C(R¹³)═C(R¹³)--,

3) --C═C(R¹³)--N═C(R¹³)--N═C(R¹³)--,

4) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═N--, or

5) --C═N--C(R¹³)═N--C(R¹³)═C(R¹³)--; ##STR26## is as defined above; ##STR27## is as defined above; or ##STR28## wherein G is S; R² is

a) --(C₁ -C₁₂ alkyl)--X, or ##STR29## X is a) halogen (F, Cl, Br, I),

b) --CN,

c) --NHR¹⁴

d) --NHC(NH)H,

e) --NHC(NH)NHR¹⁴,

f) --C(NH)NHR¹⁴,

g) --OR¹⁴, or

h) --SC(═NH)NHR¹⁴ ;

R¹¹ is H;

R¹³ is

H, halogen (F, Cl, Br, I), --(CH₂)_(w) NO₂, C₁ -C₆)alkyl, --(CH₂)_(r) --D, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NR⁸ R³, --(CH₂)_(w) S (O)₂ R⁷, --(CH₂)_(w) SO₂ NHCO--(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ -phenyl--(CH₂)_(w) SO₂ NH--(C₁ -C₅)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NHCO₂ (C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) CN⁴ H, --O(C═O)--(C₁ -C₅ -alkyl), --O(CH₂)_(t) CN, --NH (CH₂)_(t) CN, --S (CH₂)_(t) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), or --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸ ;

R¹⁴ is --H;

R¹⁸ and R¹⁹ are independently

H, halo (F, Cl, Br, I), C₁ -C₆ -alkyl, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, (CH₂)_(w) S (O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) SO₂ NH--(C₁ -C₅)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(C═O)--(C₁ -C₅ -alkyl), --O(CH₂)_(t) CN, --NH (CH₂)_(t) CN, --S (CH₂)_(t) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -phenyl), or --O(C═O)phenyl;

R¹⁸ and R¹⁹ can be taken together to form a methylenedioxy group;

R²⁰ is selected from the group consisting of:

(CH₂)_(r) --D, or --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸ ;

and all other required substituents of formula (I) are defined as in Claim 3.

Specifically preferred are those most preferred compounds listed below:

N¹ -(4-phenylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(3-phenoxybenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(1-fluorenonyl)-(R)-boroarginine, hydrochloride

N¹ -(4- 1-butyl!benzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-benzoylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(5-phenyl-2-furoyl)-(R)-boroarginine, hydrochloride

N¹ -(3- N-benzyloxycarbonyl-N-methylamino!-4- 1-butyl!-benzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-phenyl-4-isoquinoloyl)-(R)-boroarginine, hydrochloride

N¹ -(4-cyclohexylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-phenylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ - 4-phenyl-2-nitrobenzoyl!boroArg, (+)-pinanediol ester

N¹ - 4-phenyl-2-fluorobenzoyl!boroArg, (+)-pinanediol ester

N¹ - 4-phenyl-2-aminobenzoyl!boroArg, (+)-pinanediol ester

N¹ - 4-phenyl-2-(methylsulfonamido)benzoyl!boroArg, (+)-pinanediol ester

N¹ - 4-phenyl-2-(cyanomethylamino)benzoyl!boroArg, (+)-pinanediol ester

N¹ - 4-phenyl-2-(cyanomethyl)benzoyl!boroArg, (+)-pinanediol ester

N¹ - 4-phenyl-2-(diethylamino)benzoyl!boroArg, (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)pinanediol ester

N¹ - 4- 2-(aminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)pinanediol ester

N¹ - 4- 2-(methoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!benzoyl!boroArg, (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!benzoyl!boroArg-OH

N¹ - 4- 2-(n-butoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)-pinanediol ester

N¹ - 4- 2-(diethylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg, (+)pinanediol ester

N¹ - 4- 2-(aminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg, (+)pinanediol ester

N¹ - 4- 2-(methoxycarbonylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg, (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg, (+)pinanediol ester

N¹ - 4- 2-(aminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg, (+)pinanediol ester

N¹ - 4- 2-(methoxycarbonylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg, (+)-pinanediol ester

N¹ -(3-phenylbenzoyl)boroarg, (+)-pinanediol

N¹ - 4-(3-BOCNHphenyl)₂ -methylbenzoyl!boroarg, (+)-pinanediol

N¹ -(5-phenyl-2-furoyl)boroarg, (+)-pinanediol

N¹ -(5-phenyl-2-thienyl)boroarg, (+)-pinanediol

N¹ - 4-(3-nitrophenyl)benzoyl!boroarg, (+)-pinanediol

N¹ - 4-(3-aminophenyl)benzoyl!boroarg, (+)-pinanediol

N¹ -(3-phenylbenzoyl)borolys, (+)-pinanediol

N¹ -(5-phenyl-2-furoyl)boroarg-OH

N¹ -(3-phenylbenzoyl)boroIrg, (+)-pinanediol

(R)- 5-amino-1- 5-(phenylmethyl)-1H-1,2,4-triazol-1-yl!acetyl!amino!-pentyl!boronic acid hydrochloride

3aS- 2(S*),3aα,4β,6β!!-(1,1-dimethylethyl) 3- 5- 4- (amino-iminomethyl)amino!-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzo-dioxaborol-2-yl)butyl!amino!carbonyl!-2-thienyl!phenyl!carbamate hydrochloride

3aS- 2(S*),3aα,4β,6β,7aα!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-5-(phenyl-methyl)-3-(2H-tetrazol-5-ylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

3aS- 2(S*),3a,4β,6β,7aα!!-1- 2- 5-amino-1-(hexahydro-3a, 5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2 -yl) pentyl!amino!-2-oxoethyl!-5-(phenylmethyl)-1H-1,2,4-triazole-3-acetic acid hydrochloride 1:1 with 3aS- 2(S*), 3aα,4β,6β,7aα!!-1- 2- 5-amino-1-(hexahydro-3a, 5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!amino!-2-oxoethyl!-3-(phenylmethyl)-1H-1,2,4-triazole-5-acetic acid hydrochloride

3aS- 2(S*),3aα,4β,6β,7aα!!-methyl 1- 2- 5-amino-1-(hexahydro-3a, 5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-amino!-2-oxoethyl!-5-(phenylmethyl)-1H-1,2,4-triazole-3-acetate hydrochloride

3aS- 2(S*),3aα,4β,6β,7aα!!-methyl 1- 2- 5-amino-1-(hexahydro-3a, 5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-amino!-2-oxoethyl!-3-(phenylmethyl)-1H-1,2,4-triazole-5-acetate hydrochloride

3aS- 2(S*), 3aα,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-3-phenyl-5-(phenyl -methyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

(R)- 5-amino-1- 3-phenyl-5-(phenylmethyl)-1H-1,2,4-triazol-1-yl!acetyl!-amino!pentyl!boronic acid hydrochloride

3aS- 2(S*), 3aα,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-3-(3-nitro-phenyl)-5-(phenylmethyl)-1H-1, 2,4-triazole-1-acetamide hydrochloride

3aS- 2(S*), 3aα,4β,6β,7aβ!!-N- 4- (aminoiminomethyl)-amino!-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) butyl!-3-(3-nitrophenyl)-5-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

3aS- 2(S*),3aα,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-3,5-bis(phenyl-methyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

3aS- 2(S*),3aα,4β,6β,7aβ!!-N- 4- (aminoiminomethyl)-amino!-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)butyl!-3,5-bis(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

3aS- 2(S*),3aα,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide

(R)- 5-amino-1- 3-(phenylmethyl)-1H-1,2,4-triazol-1-yl!acetyl!amino!-pentyl!boronic acid hydrochloride

3aS- 2(S*),3aα,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-5-methyl-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

3aS- 2(R*),3aα,4β,6β!!-N- 5-amino-1-(hexahydro-3a,5,5-tri-methyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-5- (phenyl-methoxy).sub.m ethyl!-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

3aS- 2(S*),3aα,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-5-(cyanomethyl)-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

3aS- 2(S*),3aα,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-3-(phenylmethyl)-5-propyl-1H-1,2,4-triazole-1-acetamide hydrochloride

3aS- 2(S*),3aα,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-5-phenyl-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

(R)- 5-amino-1- 5-methyl-3-(phenylmethyl)-1H-1,2,4-triazol-1-yl!acetyl!-amino!pentyl!boronic acid hydrochloride

3aS- 2(S*), 3aα,4β,6β,7β!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-3-phenyl-1H-1,2,4-triazole-1-acetamide hydrochloride

3aS- 2(S*), 3aα,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a, 5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-5-methyl -3-phenyl -1H-1,2,4-triazole-1-acetamide hydrochloride

3aS- 2(S*), 3aα,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-5-(2-phenyl-ethyl)-1H-1,2,4-triazole-1-acetamide

(R)- 5-amino-1- 5-(2-phenylethyl)-1H-1,2,4-triazol-1-yl!acetyl!amino!-pentyl!boronic acid hydrochloride

3aS- 2(S*),3aα,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-3,5-bis(2-phenyl-ethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

(R)- 5-amino-1- 3,5-bis(2-phenylethyl)-1H-1,2,4-triazol-1-yl!acetyl!amino!-pentyl!boronic acid hydrochloride

3aS- 2(S*), 3aα,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-3-(2-phenylethyl)-1H-1,2,4-triazole-1-acetamide

(R)- 5-amino-1- 3-(2-phenylethyl)-1H-1,2,4-triazol-1-yl!acetyl!amino!-pentyl!boronic acid hydrochloride

3aS- 2(S*), 3aα,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl!-3-(3-phenyl-propyl)-1H-1,2,4-triazole-1-acetamide

(R)- 5-amino-1- 5-(3-phenylpropyl)-1H-1,2,4-triazol-1-yl!acetyl!amino!-pentyl!boronic acid hydrochloride

(R)- 5-amino-1- 3-(3-phenylpropyl)-1H-1,2,4-triazol-1-yl!acetyl!amino!-pentyl!boronic acid hydrochloride

3aS- 2(S*),3aα,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-1,5-bis(phenyl-methyl)-1H-1,2,4-triazole-3-acetamide hydrochloride 2:8 with (R)- 5-amino-1- 1,5-bis(phenylmethyl)-1H-1,2,4-triazol-3-yl!acetyl!amino!-pentyl!boronic acid hydrochloride

3aS- 2(S*),3aα,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-4-methyl-2-phenyl-5-pyrimidinecarboxamide hydrochloride

3aS- 2(S*),3aα,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-2,4-diphenyl-5-pyrimidinecarboxamide hydrochloride

3aS- 2(S*),3aα,4β,6β,7aβ!!-N- 4- (amimoiminomethyl)amino!-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)-butyl!-4-methyl-2-phenyl-5-pyrimidinecarboxamide hydrochloride

3aS- 2(S*),3α,4β,6β,7aβ!!-N- 5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl!-6-phenyl-3-pyridinecarboxamide hydrochloride

(R)- 5-amino-1- (6-phenyl-3-pyridinyl)carbonyl!amino!pentyl!boronic acid dihydrochloride

Illustrative of the compounds of this invention are the following:

N¹ -(4-phenylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(3-phenylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(3-phenoxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4- 4-pyridyl!benzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-benzoylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(3-benzoylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-benzoylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(3- N-benzyloxycarbonyl!aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(3- N-benzyloxycarbonyl-N-methyl!aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-ethylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-n-propylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-isopropylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-n-butylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-tert-butylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-n-hexylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-cyclohexylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2- N-(2-phenylethyl)carbonyl!aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-n-butyloxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4- N-cyclopropylcarbonyl!aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4- N-cyclohexylcarbonyl!aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4- N-(4-methoxy)benzoyl!aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4- 4-methoxy!phenylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2- 2-phenyl!benzyloxycarbonylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2- 1-naphthyl!benzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4- 4-carboxy!phenylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-phenylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(3-phenylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(3-phenoxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-benzoylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(3-benzoylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-benzoylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(3- N-benzyloxycarbonyl!aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(3- N-benzyloxycarbonyl-N-methyl!aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-ethylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-n-propylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-isopropylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-n-butylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-tert-butylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-n-hexylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-cyclohexylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2- N-(2-phenylethyl)carbonyl!aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-n-butyloxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4- N-cyclopropylcarbonyl!aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4- N-cyclohexylcarbonyl!aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4- N-(4-methoxy)benzoyl!aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4- 4-methoxy!phenylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2- 2-phenylbenzyloxycarbonyl!benzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2- 1-naphthyl!benzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4- 4-carboxy!phenylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -( 2-anthraquinonyl!carbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -( 2-dioxothioxanthinonyl!carbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -( 2-anthraquinonyl!carbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -( 2-dioxothioxanthinonyl!carbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -( 2-fluoren-9-onyl!carbonyl)-(R)-borothiohomoarginine (+)-pinanediol, hydrobromide

N¹ -( 2-fluoren-9-onyl!carbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -( 2-fluoren-9-onyl!carbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -( 3-fluoren-9-onyl!carbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -( 3-fluoren-9-onyl!carbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -( 4-fluoren-9-onyl!carbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -( 4-fluoren-9-onyl!carbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(1-naphthoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(1-naphthoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-methoxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-carboxamidobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-fluorobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-trifluoromethylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-chlorobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-hydroxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-methoxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-carboxamidobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-fluorobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-trifluoromethylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-chlorobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-hydroxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2- 5-phenyl!furylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2- 5-phenyl!thiophen-ylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2- 5-phenyl!furylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2- 5-phenyl!thiophen-ylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(3- 6-phenyl!pyridylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(3- 5-benzyloxy!pyridylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(3- 6-phenyl!pyridylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(3- 5-benzyloxy!pyridylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-benzopyronylcarbonyl)-(R)-boroarginine(+)-pinanediol, bisulfite

N¹ -(2-benzopyronylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(3-isoquinolinylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(3-isoquinolinylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-isoquinolinylcarbonyl)-(R)-boroarginine(+)-pinanediol, bisulfite

N¹ -(2-isoquinolinylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-phenylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(3-phenylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(3-phenoxybenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4- 4-pyridyl!benzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-benzoylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(3-benzoylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-benzoylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(3- N-benzyloxycarbonyl!aminobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(3- N-benzyloxycarbonyl-N-methyl!aminobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-ethylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-n-propylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-isopropylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-tert-butylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-n-hexylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-cyclohexylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2- N-(2-phenylethyl)carbonyl!aminobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-n-butyloxybenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4- N-cyclopropylcarbonyl!aminobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4- N-cyclohexylcarbonyl!aminobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4- N-(4-methoxy)benzoyl!aminobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4- 4-methoxy!phenylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2- 2-phenyl!benzyloxycarbonylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2- 1-naphthyl!benzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4- 4-carboxy!phenylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -( 2-anthraquinonyl!carbonyl)-(R)-boroarginine, hydrochloride

N¹ -( 2-dioxothioxanthinonyl!carbonyl)-(R)-boroarginine, hydrochloride

N¹ -( 2-fluoren-9-onyl!carbonyl)-(R)-boroarginine, hydrochloride

N¹ -( 3-fluoren-9-onyl!carbonyl)-(R)-boroarginine, hydrochloride

N¹ -(1-naphthoyl)-(R)-boroarginine, hydrochloride

N¹ -( 4-fluoren-9-onyl!carbonyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-methoxybenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-carboxamidobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-fluorobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-trifluoromethylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-chlorobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-hydroxybenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2- 5-phenyl!furylcarbonyl)-(R)-boroarginine, hydrochloride

N¹ -(2- 5-phenyl!thiophen-ylcarbonyl)-(R)-boroarginine, hydrochloride

N¹ -(2-benzopyronylcarbonyl)-(R)-boroarginine, hydrochloride

N¹ -(2-isoquinolinylcarbonyl)-(R)-boroarginine, hydrochloride

N¹ -(3-isoquinolinylcarbonyl)-(R)-boroarginine, hydrochloride

N¹ -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-boroarginine, hydrochloride

N¹ -(4-phenylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(3-phenylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(3-phenoxybenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-benzoylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(3-benzoylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-benzoylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(3- N-benzyloxycarbonyl!aminobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(3- N-benzyloxycarbonyl-N-methyl!aminobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-ethylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-n-propylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-isopropylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-n-butylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-tert-butylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-n-hexylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-cyclohexylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2- N-(2-phenylethyl)carbonyl!aminobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-n-butyloxybenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4- N-cyclopropylcarbonyl!aminobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4- N-cyclohexylcarbonyl!aminobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4- N-(4-methoxy)benzoyl!aminobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4- 4-methoxy!phenylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2- 2-phenylbenzyloxycarbonyl!benzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2- 1-naphthyl!benzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4- 4-carboxy!phenylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ - (2-anthraquinonyl!carbonyl)-(R)-borothioarginine, hydrochloride

N¹ - (2-dioxothioxanthinonyl!carbonyl)-(R)-borothioarginine, hydrochloride

N¹ - (2-fluoren-9-onyl!carbonyl)-(R)-borothiohomoarginine, hydrochloride

N¹ - (2-fluoren-9-onyl!carbonyl)-(R)-borothioarginine, hydrochloride

N¹ - (3-fluoren-9-onyl!carbonyl)-(R)-borothioarginine, hydrochloride

N¹ - (4-fluoren-9-onyl!carbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(1-naphthoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-methoxybenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-carboxamidobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-fluorobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-trifluoromethylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-chlorobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-hydroxybenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2- 5-phenyl!furylcarbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(2- 5-phenyl!thiophenylcarbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(3- 6-phenyl!pyridylcarbonyl)-(R)-boroarginine, hydrochloride

N¹ -(3- 5-benzyloxy!pyridylcarbonyl)-(R)-boroarginine, hydrochloride

N¹ -(3- 6-phenyl!pyridylcarbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(3- 5-benzyloxy!pyridylcarbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-benzopyronylcarbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(3-isoquinolinylcarbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-isoquinolinylcarbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-phenylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(3-phenylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(3-phenoxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4- 4-pyridyl!benzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-benzoylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(3-benzoylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-benzoylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(3- N-benzyloxycarbonyl!aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(3- N-benzyloxycarbonyl-N-methyl!aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-ethylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-n-propylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-isopropylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-tert-butylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-n-hexylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-cyclohexylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2- N-(2-phenylethyl)carbonyl!aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-n-butyloxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4- N-cyclopropylcarbonyl!aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4- N-cyclohexylcarbonyl!aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4- N-(4-methoxy)benzoyl!aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4- 4-methoxy!phenylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2- 2-phenyl!benzyloxycarbonylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2- 1-naphthyl!benzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4- 4-carboxy!phenylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -( 2-anthraquinonyl!carbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -( 2-dioxothioxanthinonyl!carbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -( 2-fluoren-9-onyl!carbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -( 3-fluoren-9-onyl!carbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(1-naphthoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -( 4-fluoren-9-onyl!carbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-methoxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-carboxamidobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-fluorobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-trifluoromethylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-chlorobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-hydroxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2- 5-phenyl!furylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2- 5-phenyl!thiophen-ylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-benzopyronylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-isoquinolinylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(3-isoquinolinylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-phenylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(3-phenylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(3-phenoxybenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4- 4-pyridyl!benzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-benzoylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(3-benzoylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-benzoylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(3- N-benzyloxycarbonyl!aminobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(3- N-benzyloxycarbonyl-N-methyl!aminobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-ethylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-n-propylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-isopropylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-tert-butylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-n-hexylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-cyclohexylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2- N-(2-phenylethyl)carbonyl!aminobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-n-butyloxybenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4- N-cyclopropylcarbonyl!aminobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4- N-cyclohexylcarbonyl!aminobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4- N-(4-methoxy)benzoyl!aminobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4- 4-methoxy!phenylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2- 2-phenyl!benzyloxycarbonylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2- 1-naphthyl!benzoyl)-(R)-borolysine, hydrochloride

N¹ -(4- 4-carboxy!phenylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -( 2-anthraquinonyl!carbonyl)-(R)-borolysine, hydrochloride

N¹ -( 2-dioxothioxanthinonyl!carbonyl)-(R)-borolysine, hydrochloride

N¹ -( 2-fluoren-9-onyl!carbonyl)-(R)-borolysine, hydrochloride

N¹ -( 3-fluoren-9-onyl!carbonyl)-(R)-borolysine, hydrochloride

N¹ -(1-naphthoyl)-(R)-borolysine, hydrochloride

N¹ -( 4-fluoren-9-onyl!carbonyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-methoxybenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-carboxamidobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-fluorobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-trifluoromethylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-chlorobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4- 4-carboxy!phenyl-5-hydroxybenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2- 5-phenyl!furylcarbonyl)-(R)-borolysine, hydrochloride

N¹ -(2- 5-phenyl!thiophenylcarbonyl)-(R)-borolysine, hydrochloride

N¹ -(2-benzopyronylcarbonyl)-(R)-borolysine, hydrochloride

N¹ -(2-isoquinolinylcarbonyl)-(R)-borolysine, hydrochloride

N¹ -(3-isoquinolinylcarbonyl)-(R)-borolysine, hydrochloride

N¹ -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-phenylbenzoyl-R-borolysine, hydrochloride

N¹ -(2-methyl-4-phenylbenzoyl-R-borolysine, (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-phenylbenzoyl-R-borothioarginine, hydrobromide

N¹ -(2-methyl-4-phenylbenzoyl-R-borothioarginine, (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-phenylbenzoyl-R-boroarginine, hydrochloride

N¹ -(2-methyl-4-phenylbenzoyl-R-boroarginine, (+)-pinanediol, bisulfite

N¹ - 4-phenyl-2-nitrobenzoyl!boroArg(Me), (+)-pinanediol ester

N¹ - 4-phenyl-2-fluorobenzoyl!boroArg(Me), (+)-pinanediol ester

N¹ - 4-phenyl-2-aminobenzoyl!boroArg(Me), (+)-pinanediol ester

N¹ - 4-phenyl-2-(methylsulfonamido)benzoyl!boroArg(Me), (+)-pinanediol ester

N¹ - 4-phenyl-2-(cyanomethylamino)benzoyl!boroArg(Me), (+)-pinanediol ester

N¹ - 4-phenyl-2-(cyanomethyl)benzoyl!boroArg(Me), (+)-pinanediol ester

N¹ - 4-phenyl-2-(diethylamino)benzoyl!boroArg(Me), (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg (Me), (+) pinanediol ester

N¹ - (4- 2-(aminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg (Me), (+) pinanediol ester

N¹ - 4- 2-(methoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg(Me), (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!benzoyl!boroArg(Me), (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!benzoyl!boroArg(Me)--OH

N¹ - 4- 2-(n-butoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg(Me), (+)-pinanediol ester

N¹ - 4- 2-(diethylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg(Me), (+)pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg(Me), (+)pinanediol ester

N¹ - 4- 2-(aminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg(Me), (+)pinanediol ester

N¹ - 4- 2-(methoxycarbonylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg(Me), (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg(Me), (+)pinanediol ester

N¹ - 4- 2-(aminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg(Me), (+)pinanediol ester

N¹ - 4- 2-(methoxycarbonylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg(Me), (+)-pinanediol ester

N¹ - 4-phenyl-2-nitrobenzoyl!boroMPG, (+)-pinanediol ester

N¹ - 4-phenyl-2-fluorobenzoyl!boroMPG, (+)-pinanediol ester

N¹ - 4-phenyl-2-aminobenzoyl!boroMPG, (+)-pinanediol ester

N¹ - 4-phenyl-2-(methylsulfonamido)benzoyl!boroMPG, pinanediol ester

N¹ - 4-phenyl-2-(cyanomethylamino)benzoyl!boroMPG, (+)-pinanediol ester

N¹ - 4-phenyl-2-(cyanomethyl)benzoyl!boroMPG, (+)-pinanediol ester

N¹ - 4-phenyl-2-(diethylamino)benzoyl!boroMPG, (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroMPG, (+)pinanediol ester

N¹ - 4- 2-(aminosulfonyl)phenyl!-2-methyl-benzoyl!boroMPG, (+)pinanediol ester

N¹ - 4- 2-(methoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroMPG, (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!benzoyl!boroMPG, (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!benzoyl!boroMPG--OH

N¹ - 4- 2-(n-butoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroMPG, (+)-pinanediol ester

N¹ - 4- 2-(diethylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroMPG, (+)pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroMPG, (+)pinanediol ester

N¹ - 4- 2-(aminosulfonyl)phenyl!-2-fluoro-benzoyl!boroMPG, (+)pinanediol ester

N¹ - 4- 2-(methoxycarbonylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroMPG, (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroMPG, (+)pinanediol ester

N¹ - 4- 2-(aminosulfonyl)phenyl!-2-nitro-benzoyl!boroMPG, (+)pinanediol ester

N¹ - 4- 2-(methoxycarbonylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroMPG, (+)-pinanediol ester

N¹ - 4-phenyl-2-nitrobenzoyl!boroACA, (+)-pinanediol ester

N¹ - 4-phenyl-2-fluorobenzoyl!boroACA, (+)-pinanediol ester

N¹ - 4-phenyl-2-aminobenzoyl!boroACA, (+)-pinanediol ester

N¹ - 4-phenyl-2-(methylsulfonamido)benzoyl!boroACA, (+)-pinanediol ester

N¹ - 4-phenyl-2-(cyanomethylamino)benzoyl!boroACA, (+)-pinanediol ester

N¹ - 4-phenyl-2-(cyanomethyl)benzoyl!boroACA, (+)-pinanediol ester

N¹ - 4-phenyl-2-(diethylamino)benzoyl!boroACA, (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroACA, (+)pinanediol ester

N¹ - 4- 2-(aminosulfonyl)phenyl!-2-methyl-benzoyl!boroACA, (+)pinanediol ester

N¹ - 4- 2-(methoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroACA, (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!benzoyl!boroACA, (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!benzoyl!boroACA-OH

N¹ - 4- 2-(n-butoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroACA, (+)-pinanediol ester

N¹ - 4- 2-(diethylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroACA, (+)pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroACA, (+)pinanediol ester

N¹ - 4- 2-(aminosulfonyl)phenyl!-2-fluoro-benzoyl!boroACA, (+)pinanediol ester

N¹ - 4- 2-(methoxycarbonylaminosulfonyl)Phenyl!⁻ 2-fluoro-benzoyl!boroACA, (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroACA, (+)pinanediol ester

N¹ - 4- 2-(aminosulfonyl)phenyl!-2-nitro-benzoyl!boroACA, (+)pinanediol ester

N¹ - 4- 2-(methoxycarbonylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroACA, (+)-pinanediol ester

N¹ - 4-phenyl-2-nitrobenzoyl!boroLys, (+)-pinanediol ester

N¹ - 4-phenyl-2-fluorobenzoyl!boroLys, (+)-pinanediol ester

N¹ - 4-phenyl-2-aminobenzoyl!boroLys, (+)-pinanediol ester

N¹ - 4-phenyl-2-(methylsulfonamido)benzoyl!boroLys, (+)-pinanediol ester

N¹ - 4-phenyl-2-(cyanomethylamino)benzoyl!boroLys, (+)-pinanediol ester

N¹ - 4-phenyl-2-(cyanomethyl)benzoyl!boroLys, (+)-pinanediol ester

N¹ - 4-phenyl-2-(diethylamino)benzoyl!boroLys, (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroLys, (+)pinanediol ester

N¹ - 4- 2-(aminosulfonyl)phenyl!-2-methyl-benzoyl!boroLys, (+)pinanediol ester

N¹ - 4- 2-(methoxycabonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroLys, (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!benzoyl!boroLys, (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!benzoyl!boroLys--OH

N¹ - 4- 2-(n-butoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroLys, (+)-pinanediol ester

N¹ - 4- 2-(diethylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroLys, (+)pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroLys, (+)pinanediol ester

N¹ - 4- 2-(aminosulfonyl)phenyl!-2-fluoro-benzoyl!boroLys, (+)pinanediol ester

N¹ - 4- 2-(methoxycarbonylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroLys, (+)-pinanediol ester

N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroLys, (+)pinanediol ester

N¹ - 4- 2-(aminosulfonyl)phenyl!-2-nitro-benzoyl!boroLys, (+)pinanediol ester

N¹ - 4- 2-(methoxyaminosulfonyl)phenyl!-2-nitro-benzoyl!boroLys, (+)-pinanediol ester.

DETAILED DESCRIPTION OF THE INVENTION

Throughout the specification, the following conventional three-letter abbreviations for amino acid residues or amino acids apply:

Ala=alanine

Arg=arginine

Asn=asparagine

Asp=aspartic acid

Cys=cysteine

Gln=glutamine

Glu=glutamic acid

Gly=glycine

His=histidine

Ile=isoleucine

Leu=leucine

Lys=lysine

Met=methionine

Phe=phenylalanine

Pro=proline

Ser=serine

Thr=threonine

Trp=tryptophan

Tyr=tyrosine

Val=valine

Irg=arginine where the guanidine is replaced with an isothiouronium (--SC(═NH)NH₂)

Arg(Me)=arginine with the guanidino group methylated

MPG=5-methoxy-propylglycine

ACA=3-(4-amino)cyclohexylalanine

The prefix "boro" indicates amino acid residues where the carboxy group is replaced by a boronic acid (Formula I, Y¹ and Y² =--OH).

The pinanediol boronic acid ester and the pinacol boronic acid ester are abbreviated "-C₁₀ H₁₆ -" and -C₆ H₁₂ -" respectively. Other illustrations of diols useful for deriving a boronic acid orthoesters are 1,2-ethanediol, 1,3-propanediol, 1,2-propanediol, 2,3-butanediol, 1,2-diisopropylethanediol, 5,6-decanediol, 1,2-dicyclohexylethanediol.

The formamidino modified amino group is abbreviated (CH═NH). For example, the formamidino analog of -boroOrn--OH {--NH--CH (CH₂)₃ --NH--CH(NH)H!B(OH)₂ } is -boroOrn(CH═NH)--OH. Analogs containing sidechain substituents are described by indicating the substituent in parenthesis following the name of the parent residue. For example the analog of boroPhenylalanine containing a meta cyano group is -boroPhe(mCN)-. N-alkyl substituents on the guanidino group of boroArg- or on the isothiouronium analogs (boroIrg) are also put in parenthesis in a similar manner.

Other abbreviations are: Z, benzyloxycarbonyl; BSA, benzene sulfonic acid; THF, tetrahydrofuran; Boc-, g-butoxycarbonyl-; Ac-, acetyl; pNA, p-nitro-aniline; DMAP, 4-N,N-dimethylaminopyridine; Tris, Tris(hydroxymethyl)aminomethane; MS, mass spectrometry; FAB/MS, fast atom bombardment mass spectrometry. LRMS(NH₃ --CI) and HRMS(NH₃ --CI) are low and high resolution mass spectrometry, respectively, using NH₃ as an ion source

As used herein, the structure ##STR30## wherein J is N or C and K, L, M and Q are independently selected at each occurrence from the group consisting of N, CR¹³, S or O, provided that:

i) there may be only one S or O present in the ring at a time;

ii) there may only be 1-2N present when there is an O or S present;

iii) there may be only 1-4N present; is used as a substituent definition for R¹. This substituent may be exemplified by the following structures where --J--K--L--M--Q-- is:

1) --N--C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--,

2) --N--C(R¹³)═C(R¹³)--C(R¹³)═N--,

3) --N--C(R¹³)═C(R¹³)--N═C(R¹³)--,

4) --N--C(R¹³)═N--C(R¹³)═N--,

5) --N--C(R¹³)═C(R¹³)--N═N--

6) --N--C(R¹³)═N--N═N--,

7) --N--N═C(R¹³)--N═N--,

8) ═C--O--C(R¹³)═N--C(R¹³)═,

9) --C═C(R¹³)--O--C(R¹³)═N--,

10) ═C--O--C(R¹³)═C(R¹³)--N═,

11) --C═C(R¹³)--C(R¹³)═N--O--,

12) ═C--C(R¹³)═C(R¹³)--O--N═,

13) --C═C(R¹³)--O--N═C(R¹³)--,

14) ═C--S--C(R¹³)═N--C(R¹³)═,

15) --C═C(R¹³)--S--C(R¹³)═N--,

16) ═C--S--C(R¹³)═C(R¹³)--N═,

17) --C═N--S--N═C(R¹³)--,

18) --C═N--S--C(R¹³)═N--,

19) ═C--S--N═C(R¹³)--N═,

20) ═C--S--C(R¹³)═C(R¹³)--C(R¹³)═,

21) --C═C(R¹³)--S--C(R¹³)═C(R¹³)--,

22) ═C--O--C(R¹³)═C(R¹³)--C(R¹³)═, or

23) --C═C(R¹³)--O--C(R¹³)═C(R¹³)--.

As used herein, the structure ##STR31## wherein in W, R, T, U and V are independently selected at each occurrence from the group consiting of: CR¹³ or N, provided that there may be only 1-3N present, is used as a substituent definition for R¹. This substituent may be exemplified by the following structures where --C--W--R--T--U--V-- is:

1) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--,

2) --C═C(R¹³)--N═C(R¹³)--C(R¹³)═C(R¹³)--,

3) --C═C(R¹³)--C(R¹³)═N--C(R¹³)═C(R¹³)--,

4) --C═N--N═C(R¹³)--C(R¹³)═C(R¹³)--,

5) --C═C(R¹³)--N═N--C(R¹³)═C(R¹³)--,

6) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═N--,

7) --C═N--C(R¹³)═C(R¹³)--N═C(R¹³)--,

8) --C═N--C(R¹³)═N--C(R¹³)═C(R¹³)--,

9) --C═C(R¹³)--N═C(R¹³)--N═C(R¹³)--,

10) --C═N--C(R¹³)═N--N═C(R¹³)--,

11) --C═N--C(R¹³)═C(R¹³)--N═N--, or

12) --C═C(R¹³)--N═C(R¹³)--N═N--.

"Amino acid residues" as used herein, refers to natural or unnatural amino acids of either D- or L-configuration. Natural amino acids residues are Ala, Arg, Asn, Asp, Aze, Cys, Gln, Glu, Gly, His, Ile, Irg Leu, Lys, Met, Orn, Phe, Phe(4-fluoro), Pro, Sar, Ser, Thr, Trp, Tyr, and Val. Roberts and Vellaccio, The Peptides, Vol 5; 341-449 (1983), Academic Press, New York, discloses numerous suitable unnatural amino acids and is incorporated herein by reference for that purpose.

"Amino acids residues" also refers to various amino acids where sidechain functional groups are coupled with appropriate protecting groups known to those skilled in the art. "The Peptides", Vol 3, 3-88 (1981) discloses numerous suitable protecting groups and is incorporated herein by reference for that purpose.

The reactions of the synthetic methods claimed herein are carried out in suitable solvents which may be readily selected by one of skill in the art of organic synthesis, said suitable solvents generally being any solvent which is substantially nonreactive with the starting materials (reactants), the intermediates, or products at the temperatures at which the reactions are carried out, i.e., temperatures which may range from the solvent's freezing temperature to the solvent's boiling temperature. A given reaction may be carried out in one solvent or a mixture of more than one solvent. Depending on the particular reaction step, suitable solvents for a particular reaction step may be selected.

The compounds herein described may have asymmetric centers. All chiral, diastereomeric, and racemic forms are included in the present invention. Many geometric isomers of olefins, C═N double bonds, and the like can also be present in the compounds described herein, and all such stable isomers are contemplated in the present invention. It will be appreciated that certain compounds of the present invention contain an asymmetrically substituted carbon atom, and may be isolated in optically active or racemic forms. It is well known in the art how to prepare optically active forms, such as by resolution of racemic forms or by synthesis, from optically active starting materials. Also, it is realized that cis and trans geometric isomers of the compounds of the present invention are described and may be isolated as a mixture of isomers or as separated isomeric forms. All chiral, diastereomeric, racemic forms and all geometric isomeric forms of a structure are intended, unless the specific stereochemistry or isomer form is specifically indicated.

When any variable (for example, R¹ through R²⁰, R^(20a), m, n, D, E, F, W, X, etc.) occurs more than one time in any constituent or in Formula (I), its definition on each occurrence is independent of its definition at every other occurrence. Thus, for example, if a group is shown to be substituted with 0-3 R¹¹, then said group may optionally be substituted with up to three R¹¹ and R¹¹ at each occurrence is selected independently from the defined list of possible R¹¹. Also, for example, in -N(R¹⁵)₂, each of the R¹⁵ substituents may be independently selected from the list of possible R²⁰ groups defined. Also, combinations of substituents and/or variables are permissible only if such combinations result in stable compounds. Similarly, by way of example, for the group --C(R¹¹)₂ --, each of the two R¹¹ substituents on C is independently selected from the defined list of possible R¹¹.

As used herein, "alkyl" is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms; "haloalkyl" is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms, substituted with 1 or more halogen (for example -C_(v) F_(w) where v=1 to 3 and w=1 to (2v+1)); "alkoxy" represents an alkyl group of indicated number of carbon atoms attached through an oxygen bridge; "cycloalkyl" is intended to include saturated ring groups, including mono-,bi- or poly-cyclic ring systems, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, adamantyl and cyclooctyl; and "biycloalkyl" is intended to include saturated bicyclic ring groups such as 3.3.0!bicyclooctane, 4.3.0!bicyclononane, 4.4.0!bicyclodecane (decalin), 2.2.2!bicyclooctane, and so forth. "Alkenyl" is intended to include hydrocarbon chains of either a straight or branched configuration and one or more unsaturated carbon--carbon bonds which may occur in any stable point along the chain, such as ethenyl, propenyl, and the like; and "alkynyl" is intended to include hydrocarbon chains of either a straight or branched configuration and one or more triple carbon-carbon bonds which may occur in any stable point along the chain, such as ethynyl, propynyl and the like.

"Halo" or "halogen" as used herein refers to fluoro, chloro, bromo, and iodo; and "counterion" is used to represent a small, negatively charged species such as chloride, bromide, hydroxide, acetate, sulfate, and the like.

As used herein, "aryl" or "aromatic residue" is intended to mean phenyl or naphthyl; the term "arylalkyl" represents an aryl group attached through an alkyl bridge. By way of examples: the term "C₇ -C₁₀ arylalkyl" is intended to refer to an aryl group attached through a C₁ -C₄ alkyl bridge to the residue of the indicated compound; the term "(C₁ -C₃ alkyl)aryl" is intended to refer to a C₁ -C₃ alkyl group which is attached through an aryl ring to the residue of the indicated compound; the term "aryl(C₁ -C₃ alkyl)" is intended to refer to an aryl group attached through a C₁ -C₃ alkyl group to the residue of the indicated compound.

As used herein, "carbocycle" or "carbocyclic residue" is intended to mean any stable 3- to 8-membered monocyclic or bicyclic or 7- to 14-membered bicyclic or tricyclic or an up to 26-membered polycyclic carbon ring, any of which may be saturated, partially unsaturated, or aromatic. Examples of such carbocyles include, but are not limited to, cyclopropyl, cyclopentyl, cyclohexyl, phenyl, biphenyl, naphthyl, indanyl, adamantyl, or tetrahydronaphthyl (tetralin).

As used herein, the term "heterocycle" is intended to mean a stable 5- to 7-membered monocyclic or bicyclic or 7- to 10-membered bicyclic heterocyclic ring which is saturated and consists of carbon atoms and from 1 to 4 heteroatoms independently selected from the group consisting of N, O and S and wherein the nitrogen and sulfur heteroatoms may optionally be oxidized, and the nitrogen may optionally be quaternized, and including any bicyclic group in which any of the above-defined heterocyclic rings is fused to a benzene ring. The heterocyclic ring may be attached to its pendant group at any heteroatom or carbon atom which results in a stable structure. The term "heteroaryl" is intended to mean an aromatic form of a heterocyclic ring. Unless otherwise specified, the heterocyclic and heteroaryl rings described herein may be substituted on carbon or on a nitrogen atom if the resulting compound is stable. Unless otherwise specified, examples of such heterocycles include, but are not limited to, pyridinyl, pyrimidinyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, tetrazolyl, benzofuranyl, benzothiophenyl, indolyl, indolenyl, quinolinyl, isoquinolinyl, benzimidazolyl, piperidinyl, 4-piperidonyl, pyrrolidinyl, 2-pyrrolidonyl, pyrrolinyl, tetrahydrofuranyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, decahydroquinolinyl or octahydroisoquinolinyl, azocinyl, triazinyl, 6H-1,2,5-thiadiazinyl, 2H, 6H-1,5,2-dithiazinyl, thiophenyl, thianthrenyl, pyranyl, isobenzofuranyl, chromenyl, xanthenyl, phenoxathiinyl, 2H-pyrrolyl, isothiazolyl, isoxazolyl, pyrazinyl, pyridazinyl, indolizinyl, isoindolyl, 3H-indolyl, 1H-indazolyl, purinyl, 4H-quinolizinyl, phthalazinyl, naphthyridinyl, quinoxalinyl, quinazolinyl, cinnolinyl, pteridinyl, 4aH-carbazolyl, carbazolyl, β-carbolinyl, phenanthridinyl, acridinyl, perimidinyl, phenanthrolinyl, phenazinyl, phenarsazinyl, phenothiazinyl, furazanyl, phenoxazinyl, isochromanyl, chromanyl, imidazolidinyl, imidazolinyl, pyrazolidinyl, pyrazolinyl, piperazinyl, indolinyl, isoindolinyl, quinuclidinyl, morpholinyl, oxazolidinyl, benzotriazolyl, benzisoxazolyl, oxindolyl, benzoxazolinyl, or isatinoyl. Also included are fused ring and spiro compounds containing, for example, the above heterocycles.

When a bond to a substituent is shown to cross the bond connecting two atoms in a ring, then such substituent may be bonded to any atom on the ring. When a substituent is listed without indicating the atom via which such substituent is bonded to the rest of the compound of formula I, then such substituent may be bonded via any atom in such substituent. For example, when the substituent is piperazinyl, piperidinyl, or tetrazolyl, unless specified otherwise, said piperazinyl, piperidinyl, tetrazolyl group may be bonded to the rest of the compound of formula (I) via any atom in such piperazinyl, piperidinyl, tetrazolyl group.

Combinations of substituents and/or variables are permissible only if such combinations result in stable compounds. By stable compound or stable structure it is meant herein a compound that is sufficiently robust to survive isolation to a useful degree of purity from a reaction mixture, and formulation into an efficacious therapeutic agent.

The term "substituted", as used herein, means that an one or more hydrogen on the designated atom is replaced with a selection from the indicated group, provided that the designated atom's normal valency is not exceeded, and that the substitution results in a stable compound. When a substitent is keto (i.e., ═O), then 2 hydrogens on the atom are replaced.

As used herein, the term "any group that, when administered to a mammalian subject, cleaves to form a free hydroxyl, amino or sulfhydryl" means any group bonded to an O, N, or S atom, respectively, which is cleaved from the O, N, or S atom when the compound is administered to a mammalian subject to provide a compound having a remaining free hydroxyl, amino, or sulfhydryl group, respectively. Examples of groups that, when administered to a mammalian subject, are cleaved to form a free hydroxyl, amino or sulfhydryl, include but are not limited to, phosphate esters, C₁ -C₆ alkyl substituted with 0-3 R¹¹, C₃ -C₆ alkoxyalkyl substituted with 0-3 R¹¹, C₁ -C₆ alkylcarbonyl substituted with 0-3 R¹¹, C₁ -C₆ alkoxycarbonyl substituted with 0-3 R¹¹, C₁ -C₆ alkylaminocarbonyl substituted with 0-3 R¹¹, benzoyl substituted with 0-3 R¹², phenoxycarbonyl substituted with 0-3 R¹², phenylaminocarbonyl substituted with 0-3 R¹², or heteroarylcarbonyl. Examples of groups that, when administered to a mammalian subject, are cleaved to form a free hydroxyl, amino or sulfhydryl, may include hydroxy, amine or sulfhydryl protecting groups, respectively.

As used herein, the term "amine protecting group" means any group known in the art of organic synthesis for the protection of amine groups. Such amine protecting groups include those listed in Greene and Wuts, "Protective Groups in Organic Synthesis" John Wiley & Sons, New York (1991) and "The Peptides: Analysis, Synthesis, Biology, Vol. 3, Academic Press, New York (1981), the disclosure of which is hereby incorporated by reference. Any amine protecting group known in the art can be used. Examples of amine protecting groups include, but are not limited to, the following: 1) acyl types such as formyl, trifluoroacetyl, phthalyl, and p-toluenesulfonyl; 2) aromatic carbamate types such as benzyloxycarbonyl (Cbz) and substituted benzyloxycarbonyls, 1-(p-biphenyl)-1-methylethoxycarbonyl, and 9-fluorenylmethoxycarbonyl (Fmoc); 3) aliphatic carbamate types such as tertbutyloxycarbonyl (Boc), ethoxycarbonyl, diisopropylmethoxycarbonyl, and allyloxycarbonyl; 4) cyclic alkyl carbamate types such as cyclopentyloxycarbonyl and adamantyloxycarbonyl; 5) alkyl types such as triphenylmethyl and benzyl; 6) trialkylsilane such as trimethylsilane; and 7) thiol containing types such as phenylthiocarbonyl and dithiasuccinoyl.

The term "amino acid" as used herein means an organic compound containing both a basic amino group and an acidic carboxyl group. Included within this term are natural amino acids, modified and unusual amino acids, as well as amino acids which are known to occur biologically in free or combined form but usually do not occur in proteins. Included within this term are modified and unusual amino acids,such as those disclosed in, for example, Roberts and Vellaccio (1983) The Peptides, 5: 342-429, the teaching of which is hereby incorporated by reference. Modified or unusual amino acids which can be used to practice the invention include, but are not limited to, D-amino acids, hydroxylysine, 4-hydroxyproline, an N--Cbz-protected amino acid, ornithine, 2,4-diaminobutyric acid, homoarginine, norleucine, N-methylaminobutyric acid, naphthylalanine, phenylglycine, β-phenylproline, tert-leucine, 4-aminocyclohexylalanine, N-methyl-norleucine, 3,4-dehydroproline, N,N-dimethylaminoglycine, N-methylaminoglycine, 4-aminopiperidine-4-carboxylic acid, 6-aminocaproic acid, trans-4-(aminomethyl)-cyclohexanecarboxylic acid, 2-, 3-, and 4-(aminomethyl)-benzoic acid, 1-aminocyclopentanecarboxylic acid, 1-aminocyclopropanecarboxylic acid, and 2-benzyl-5-aminopentanoic acid.

The term "peptide" as used herein means a compound that consists of two or more amino acids (as defined herein) that are linked by means of a peptide bond. The term "peptide" also includes compounds containing both peptide and non-peptide components, such as pseudopeptide or peptide mimetic residues or other non-amino acid components. Such a compound containing both peptide and non-peptide components may also be referred to as a "peptide analog".

The term "peptide bond" means a covalent amide linkage formed by loss of a molecule of water between the carboxyl group of one amino acid and the amino group of a second amino acid.

As used herein, "pharmaceutically acceptable salts" refer to derivatives of the disclosed compounds wherein the parent compound of formula (I) is modified by making acid or base salts of the compound of formula (I). Examples of pharmaceutically acceptable salts include, but are not limited to, mineral or organic acid salts of basic residues such as amines; alkali or organic salts of acidic residues such as carboxylic acids; and the like.

"Prodrugs" are considered to be any covalently bonded carriers which release the active parent drug according to formula (I) in vivo when such prodrug is administered to a mammalian subject. Prodrugs of the compounds of formula (I) are prepared by modifying functional groups present in the compounds in such a way that the modifications are cleaved, either in routine manipulation or in vivo, to the parent compounds. Prodrugs include compounds of formula (I) wherein hydroxy, amine, or sulfhydryl groups are bonded to any group that, when administered to a mammalian subject, cleaves to form a free hydroxyl, amino, or sulfhydryl group, respectively. Examples of prodrugs include, but are not limited to, acetate, formate, or benzoate derivatives of alcohol and amine functional groups in the compounds of formula (I); phosphate esters, dimethylglycine esters, aminoalkylbenzyl esters, aminoalkyl esters and carboxyalkyl esters of alcohol and phenol functional groups in the compounds of formula (I); and the like.

The pharmaceutically acceptable salts of the compounds of formula (I) include the conventional non-toxic salts or the quaternary ammonium salts of the compounds of formula (I) formed, for example, from non-toxic inorganic or organic acids. For example, such conventional non-toxic salts include those derived from inorganic acids such as hydrochloric, hydrobromic, sulfuric, sulfamic, phosphoric, nitric and the like; and the salts prepared from organic acids such as acetic, propionic, succinic, glycolic, stearic, lactic, malic, tartaric, citric, ascorbic, pamoic, maleic, hydroxymaleic, phenylacetic, glutamic, benzoic, salicylic, sulfanilic, 2-acetoxybenzoic, fumaric, toluenesulfonic, methanesulfonic, ethane disulfonic, oxalic, isethionic, and the like.

The pharmaceutically acceptable salts of the present invention can be synthesized from the compounds of formula (I) which contain a basic or acidic moiety by conventional chemical methods. Generally, such salts can be prepared by reacting the free acid or base form of these compounds with a stoichiometric amount of the appropriate base or acid in water or in an organic solvent, or in a mixture of the two; generally, nonaqueous media like ether, ethyl acetate, ethanol, isopropanol, or acetonitrile are preferred. Lists of suitable salts are found in water or in an organic nonaqueous media like ether, ethyl acetate, ethanol, isopropanol, or acetonitrile are preferred. Lists of suitable salts are found in Remington's Pharmaceutical Sciences, 17th ed., Mack Publishing Company, Easton, Pa., 1985, p. 1418, the disclosure of which is hereby incorporated by reference.

The disclosures of all of the references cited herein are hereby incorporated herein by reference in their entirety.

SYNTHESIS

The compounds of formula (I) can be prepared using the reactions and techniques described below. The reactions are performed in a solvent appropriate to the reagents and materials employed and suitable for the transformations being affected. It will be understood by those skilled in the art of organic synthesis that the functionality present on the molecule should be consistent with the chemical transformations proposed and this will sometimes require judgment as to the order of synthetic steps or selection of particular process scheme used from that shown below in order to obtain a desired compound of the invention. ##STR32##

Amine hydrochloride 1 is readily available via the procedure of Kettner and Shenvi (EP 0293881 A2).

There are numerous synthetic methods by which to prepare amide 2, however, competing with amide formation is the cyclization of 1 to afford a complex mixture containing the desired amide and the corresponding N-acylboroproline. Since purification at this stage is unfeasible, choosing the correct method for amide formation is crucial to obtaining 2 in a purity suitable for subsequent synthetic transformations.

Three methods are preferred for the preparation of 2. In the first, a solution of 1 in tetrahydrofuran or dichloromethane at 0° C. is treated sequentially with the desired acid chloride followed by two equivalents of triethylamine. The mixture is then allowed to warm to room temperature overnight. The second method is the mixed anhydride procedure of Anderson, et. al. (J. Am Chem. Soc. 1967, 89, 5012). In this method the isobutyl mixed anhydride is generated by dissolving the carboxylic acid component in tetrahydrofuran and adding one equivalent of N-methylmorpholine. The solution is cooled to 0° C. and one equivalent of isobutyl chloroformate is added. After 5 minutes, a solution of 1 in chloroform is added, followed by the addition of one equivalent of triethylamine. The mixture is typically stirred at 0° C. for one hour followed by one to several hours at room temperature. The third method for amide formation is the hydroxybenzotriazole/DCC method of Konig and Geiger (Chem. Ber. 1970, 103, 788-98). Thus, to a solution of 1 and the carboxylic acid component in dimethylformamide or tetrahydrofuran at 0° C. is added N-methylmorpholine, 1-hydroxybenzotriazole hydrate (2 eq) and DCC (1.05 eq). The solution is allowed to warm to room temperature overnight.

The preferred method for the preparation of azide 3 is by reaction of 2 with sodium azide (1.1 eq) in dimethylformamide at 70° C. for 2 hours.

The azide displacement may also be performed prior to amide formation. This is the preferred method in cases where the rate of amide formation is slow relative to the rate of cyclization. Azide 4 is prepared by a modification of the procedure of Kettner and Shenvi (EP 0293881 A2) as shown in Scheme 2. Thus, bromide 5 is reacted with sodium azide, followed by homologation to give 6, chloride displacement to afford 7 and acidic hydrolysis to give 4. Amide formation between 4 and the carboxylic acid component then affords 3 directly. ##STR33##

Reduction of azide 3 to amine 8 may be accomplished by hydrogenation over precious metal catalysts. The preferred catalyst for this transformation is Pearlman's catalyst (palladium hydroxide on carbon). The amine is typically isolated as the hydrochloride salt. Isolation of 8 as the free base typically results in lowered yields. Salts of 8 which may confer superior physical properties may be preferred over the hydrochloride salt.

Formamidination of amine 8 may be accomplished using cyanamide. Due to the low reactivity of amine 8, however, the preferred method for this transformation is reaction with 4-dimethylamin-opyridine (DMAP) and aminoiminomethanesulfonic acid (AMSA, prepared by the method of Kim, et. al., Tetrahedron Lett. 1988, 29, 3183-6). This affords guanidine 9, which is isolated as the bisulfite or hydrochloride salt.

Cleavage of pinanediol ester 9 may be accomplished using anhydrous boron trichloride according to the procedure of Matteson and Ray (J. Am. Chem. Soc. 1980, 102, 7588). This method, however, is strongly Lewis acidic and leads to partial destruction of the substrate. The preferred method for water soluble boronic acids is a transesterification reaction that is run in the presence of excess phenylboronic acid. The free boronic acid 10 may then be isolated using cation exchange chromatography.

The isothiouronium functionalized analogs 11/12 are prepared from bromide 2 according to the procedure of Kettner and Shenvi (EP 0293881 A2).

Inhibitors containing a sulfonamide in place of a carboxamide are prepared from either 1 or 4 by reaction with a sulfonyl chloride in the presence of a hindered amine (Scheme 3). The product sulfonamide 13 is then converted to the guanidinium 14 or isothiouronium 15 in the same manner as the corresponding carboxamides. ##STR34##

Inhibitors containing the borolysine moiety are prepared analogously to those containing boroarginine according to Kettner and Shenvi (EP 0293881 A2).

Novel biaryls synthesized in this invention are prepared through palladium catalyzed coupling of an appropriate arylmetal species to the aryl halide of choice using the methods described in Negishi, et. al., Org. Synth. 1987, 66, 67-74, and references cited within.

Synthetic approaches toward construction of pyrroles are numerous: R. J. Sundberg in "Comprehensive Heterocyclic Chemistry", A. R. Katritzky (Ed.), Pergamon Press, New York (1984), Vol. 4, p. 705; Synthesis, 1946, 281. The following discussion is restricted to the most common and reliable methods towards the synthesis of pyrroles within the general scope of the invention.

Compounds where R¹ is a pyrrole can be synthesized as shown on Scheme 4. ##STR35##

Starting material diketone 16 may or may not have its substituents R¹³⁻¹⁶ in final form as defined in the scope. These substituents might be in protected forms or in the form of suitable precursors which make the heterocyclic portion, for example, amenable to synthesis. These precursor forms can then be converted to their final forms later on in the synthesis using procedures familiar to one skilled in the art.

The cyclization condensation of 1,4-dicarbonyl compounds with ammonia, primary amines or related compounds, the Paal-Knorr reaction, is one of the most general and widely applicable pyrrole syntheses, R. A. Jones and G. P. Bean, "The Chemistry of Pyrroles", Academic Press, London, 1977; p. 77-81. The generality of this approach is primarily determined by the availability of the dicarbonyl precursors, 16, as illustrated by Scheme 4. By heating such diketones with ammonia or amines in a solvent like benzene, toluene or methylene chloride with a catalyst such as sulfuric acid, acetic acid, p-toluenesulfonic acid, alumina or even titanium tetrachloride, pyrroles like 17 may be prepared.

Subsequent alkylation of pyrrole 17 with a bromoester, for example, leads to the alkylated heterocycle 18. Alkylation conditions include either first deprotonating with NaH or KH in DMF followed by addition of the alkylating agent or simply stirring the heterocycle with the alkylaning agent in an inert solvent such as DMF or DMSO at 0° C. to 100° C. in the presence of an acid scavenger such as K₂ CO₃.

Saponification of ester 18 followed by coupling aminoboronic ester 1 or 19 as discussed previously yields compound 20. This bromide may be either elaborated to the lysine side-chain 21 (X=1) or if X=0, into the corresponding ornithine side-chain or any other side-chain discussed previously. Subsequent hydrolysis of the boronic ester yields the boronic acid as discussed previously too.

The cyclization of diynes 23 with amines has been reported and an adaptation of this method is shown in Scheme 5 (K. E. Schulte et al., Chem. Ber (1965) 98; A. J. Chalk Tet. Lett. (1972)₃₄₈₇). The diynes are made via transition metal catalyzed coupling of alkynes, i.e., the Cadio-Chodkiewicz reaction (W. Chodkiewicz Ann. Chim. (Paris) (1957)2 81g). ##STR36##

Furans (27) have been converted directly to pyrroles by treatment with amines but the harsh conditions required (400° C./Al₂ O₃) precludes its generality. 2,5-Dialkoxytetrahydrofurans (29) have been more commonly employed as furan (or 1,4-dicarbonyl) equivalents and react readily with aliphatic or aromatic amines (and even weakly nucleophilic sulfonamides) to give pyrroles as shown in Scheme 6 , J. W. F. Wasley and K. Chan, Synth. Commun. 3, 303 (1973). Although commercially available 2,5-dialkoxytetrahydrofurans (29) (R¹ =R² =H))generally restrict one to preparing 1-substituted pyrroles, more highly substituted systems may be obtained by a three-step alcoholysis of the appropriate furans (27) to the more highly substituted 2,5-dialkoxytetrahydrofurans (29) as shown in Scheme 6, N. L. Weinberg and H. R. Weinberg, Chem. Rev., 68, 449 (1968); N. Elming, Adv. Org. chem., 2, 67 (1960).

The Hantzsch synthesis utilizes the condensation of β-haloketones (30a) and β-ketoesters (31) in the presence of ammonia or a primary amine to give pyrroles such as (32), as shown in Scheme 7, A. Hantzsch, Chem. Ber., 23, 1474 (1980); D. C. von Beelen, J. Walters, and S. von der Gen, Rec Trav. Chem. 98, 437 (1979). Among the numerous modifications reported over the years, the substitution of (30a) with the readily available α-hydroxyaldehydes or nitroalkenes has expanded the versatility and generality of this important method, D. M. McKinnon, Can. J. Chem. 43, 2628 (1965); H. George and H. J. Roth, Arch. Pharm. 307, 699 (1974); C. A. Grok and K. Camenisch, Helv. Chem. Acta, 36, 49 (1953). ##STR37##

The closely related Knorr condensation involves the reaction between amino carbonyl compounds (or their precursors) and carbonyl (or dicarbonyl) compounds, J. M. Patterson, Synthesis, 282 (1976). Representative methods for preparing substituted pyrroles (35 and 38) are shown by Scheme 8, equations a) and b), S. Umio et al., Jap. Pat. 7018653, Fujisawa Pharmaceutical Co., Ltd., 1970 (C.A. 73, 77039, 1970); K. Tanaka, K. Kariyone, S. Umio, Chem. Phram. Bull (Tokyo)), 17, 611 (1969).

The elaboration of an appropriately functionalized pyrrole is another method for preparing pyrroles of general formula I. Methyl (or ethyl) 5-formyl-1H-pyrrole-2-carboxylate (43) is a particularly useful intermediate with regards to pyrroles claimed in this invention and has been prepared by a number of methods as shown by Scheme 9, eq. a, W. A. Davies, A. R. Pinder and I. G. Morris, Tetrahedron 18, 405 (1962); Org Syn., vol 36, p. 74; Org. Syn., vol. 51.

More recently, Ullrich has extended the Vilsmeyer-Haack formylation of pyrroles to include vinylogous systems such as (46) by using the 3-(N,N-dimethylformamide derivative, as shown by Scheme 9, eq. b, F. W. Ullrich and E. Breitmaier, Synthesis, 641 (1983); W. Heinz, et al., Tetrahedron, 42, 3753 (1986).

An especially attractive approach to pyrroles claimed in this invention has recently been reported, whereby lithiation of the 6-dimethylamino-1-azafulvene dimer (49) followed by treatment with an appropriate electrophile and subsequent hydrolysis leads to 5-substituted pyrrole-2-carboxaldehydes (51), as illustrated in Scheme 10, J. M. Muchowski and P. Hess, Tetrahedron Lett, 29, 777 (1988). The carboxylic acid, ester and aldehyde side-chains depicted in Schemes 9-10 can be readily converted to R¹³⁻¹⁶ by methods familiar to one skilled in the art. ##STR38##

A general and versatile approach to pyrazoles (R¹ =pyrazole) involves condensation of a 1,3-difunctional compound (usually dicarbonyl) with hydrazine or its derivatives, as shown in Scheme 11 for pyrazoles of the formula 53 and reviewed by G. Corspeau and J. Elguerv, Bull. Soc. Chim. Fr., 2717 (1970). Rarely have pyrazoles have been prepared in which the N--N bond is the last step of the ring closure, J. Elguerv in Comprehensive Heterocyclic Chemistry, S. R. Katritzky (Ed.) Pergamon Press, New York, Vol. 5 (1984), p. 274; J. Barluenga, J. Chem. Soc, Perkin Trans.1, 2275 (1983). ##STR39##

The condensation of 1,3-dicarbonyl compounds with hydrazine hydrate derivatives is generally carried out by admixture of the two components in a suitable solvent like a lower alcohol, ether, or THF at 0° C. to the reflux temperature for 1-18 hours.

The synthesis of 1,3-dicarbonyl compounds has received considerable attention in the literature and most of the major approaches towards 1,3-diketones 52 of interest in this invention are illustrated by Scheme 12. ##STR40##

Esters 54a can be reacted with ketones 54 using bases like sodium ethoxide, sodium hydride or sodium amide in a suitable solvent like alcohol, DMF, DMSO or benzene at 0° C. to reflux for 4-18 hours with 30-70% efficiency, J. M. Sprague, Lo J. Beckham and H. Adkins, J. Amer. Chem. Soc., 56, 2665 (1934). Metallation of hydrazines 55with n-BuLi followed by reaction with carboxylic acid chlorides and subsequent hydrolysis affords 52, D. Enders and P. Wenster, Tetrahedron Lett., 2853 (1978). Metallation of 54 with the non-nucleophilic mesityl lithium followed by acylation also affords 52, A. K. Beck, M. S. Hoelstein and D. Seebach, Tetrahedron Lett., 1187 (1977); D. Seebach, Tetrahedron Lett., 4839; (1976).

As shown in Scheme 12, equation b, the addition of Grignard reagents to β-keto carboxylic acid chlorides may be limited to monoaddition at low temperatures to provide 52, C. D. Hurd and G. D. Kelso, J. Amer. Amer. Soc. 62, 1548 (1940); F .Sato, M. Trone, K. Oyuro, and M. Sato, Tetrahedron Lett. 4303 (1979). Lithium dialkyl copper reagents (R² CuLi) have also been used, Luong-Thi and Riviero, J. Organomet. Chem. 77, C52 (1974). Analogously, addition of alkyllithium reagents (R¹⁵ Li) to the monoanions of β-keto esters 57 also give rise to 1,3-diketones, S. N. Huckin and L. Weiler, Can. J. Chem. 52, 1379 (1974).

Eschenmoser has demonstrated a synthesis of β-diketones through a sulfur extrusion reaction of keto thioesters 58 with tributylphosphine, triethylamine and lithium perchlorate, S. Eshenmoser, Helv. Chim. Acta., 54, 710 (1971).

The rearrangement of α,β-epoxy ketones 59 to β-diketones 52 catalyzed by Pd° has been reported, R. Noyori, J. Amer. Chem. Soc. 102, 2095 (1980).

Mixed anhydrides such as 61, available from carboxylic acids 60 and trifluoroacetic anhydride, have been shown to acylate alkynes 62 to produce the enol trifluoroacetate of a β-diketone 63. Transesterification by refluxing with methanol liberates the β-diketone 52, A. L. Henne and J. M. Tedder, J. Chem. Soc. 3628 (1953). ##STR41##

Compounds where R¹ 50 imidazole, such as 65, are readily available by any of a number of standard methods. For example, acylaminoketone 64 can be cyclized with ammonia or equivalents thereof, D. Davidson, et al., J. Org. Chem., 2, 319 (1937) to the to corresponding imidazole as shown in Scheme 13. The corresponding oxazole 66 can also be converted to imidazole 65 by action of ammonia or amines in general, H. Bredereck, et. al., Ber., 88, 1351 (1955); J. W. Cornforth and R. H. Cornforth, J. Chem. Soc., 96, (1947).

Several alternative routes to imidazoles 65 are illustrated in Scheme 14. As shown in Scheme 14 equation a), reaction of the appropriate R¹³ substituted imidate esters 67 with an appropriately substituted α-hydroxy- or α-haloketone or aldehyde 68 in ammonia leads to imidazoles of formula 65, P. Dziuron, and W. Schunack, Archive, Pharmaz., 307 and 470 (1974).

The starting imidazole compounds 65 wherein R¹³ is hydrogen can be prepared as shown in equation b) by reaction of the appropriate R¹³ -substituted imidate ester 67 with α-aminoacetaldehyde dimethyl acetal, M. R. Grimmett, Adv. Heterocyclic Chem., 12, 103 (1970).

As shown in equation c), imidazole 72 (wherein R¹³ =hydrogen and CH₂ OH) can be prepared by treatment of the imidate ester 67 with 1,3-dihydroxyacetone 71 in ammonia by the procedure described in Archive der Pharmazie, 307, 470 (1974). Halogenation of imidazole 72 or any imidazole wherein R¹³ is hydrogen is preferably accomplished by reaction with one to two equivalents of N-halosuccinimide in a polar solvent such as dioxane or 2-methoxyethanol at a temperature of 40°-100° C. for 1-10 hours.

Compounds of formula 73 can also be prepared from 70 by reaction with formaldehyde as described in E. F. Godefroi, et al., Recueil, 91, 1383 (1972) followed by halogenation as was described above.

As shown in equation d) the imidazoles 65 can also be prepared by reaction of R¹³ substituted amidines 74 with an α-hydroxy- or α-haloketone or aldehyde 68 as described by F. Kunckel, Ber., 34, 637, (1901).

As shown in equation e), preparation of the nitroimidazoles (65, R¹³ =NO₂) is preferably accomplished by heating the appropriate starting imidazole in a 3:1 mixture of conc. sulfuric acid/conc. nitric acid at 60°-100° C. for 1-6 hours. Nitration of the imidazole can be achieved by first converting the hydroxmethylimidazole to the corresponding chloromethylimidazole 75 employing thionyl chloride or oxalyl chloride. Nitration, as described above, followed by hydrolysis provides the nitroimidazoles 77.

Imidazoles 80 where R¹³ =CN can be prepared as shown in equation f) by reaction of R¹³ substituted ortho esters, ortho acids or aldehydes (followed by oxidation of the aldehyde) with diaminomaleonitrile 79 by the procedure described by R. W. Begland et al., J. Org. Chem., 39, 2341 (1974). Likewise, R¹³ substituted imidate esters 67 also react with diaminomaleonitrile to give 4,5-dicyanoimidazoles 80. The nitrile groups can be further elaborated into other functional groups by methods familiar to one skilled in the art.

Compounds wherein R¹³ =alkyl of 1-6 (straight or branched), phenyl, phenalkyl where alkyl is 1-3 carbon atoms, etc. and another R¹³ =CH₂ OH can be prepared as shown in equation g). The imidazoles 83 were prepared as described in L A. Reiter, J. Org. Chem., 52, 2714 (1987), Hydroxymethylation of 83 as described by U. Kempe, et al. in U.S. Pat. No. 4,278,801 provides the hydroxymethylimidazoles 84.

The CH₂ OH group, as in imidazolemethanol 72, is a versatile synthon for other functional groups. Scheme 15 shows some of these transformations, all of which are familiar to one skilled in the art. ##STR42##

A suitably protected imidazole 85 may undergo selective halogen-metal exchange followed by quenching 5 with electrophiles to yield trisubstituted imidazoles (Scheme 16) (M. Groziak and L. Wei J. Org. Chem. (1992) 57, 3776). This strategy can be used to add several R¹³ groups onto the imidazole ring. By changing the order in which the electrophiles are added, one may change the position to which the electrophile gets attached onto the imidazole ring. ##STR43## where (R¹³)+ is a suitable electrophilic precursors to R¹³.

The pyrazoles and imidazoles disclosed previously and other heterocycles which will be mentioned later in this specification may undergo alkylation onto a nitrogen ##STR44## atom just as the pyrrole in Scheme 4 by simply stirring a mixture of the heterocycle 88 and alkylbromide, iodide, mesylate or tosylate 89 in the presence of an acid scavanger such as potassium carbonate in an inert solvent such as THF or DMF for several hours to several days at room temperature or up to the reflux temperature of the solvent (Scheme 17).

Another way to make 9Q involves first deprotonation of the N--H of heterocycle 88 with a base such as NaH, KH, n-BuLi, t-BuLi, etc., followed by displacement of the X-leaving group of 89 to yield 90.

This sequence can be performed in inert solvents such as ether or THF. NaH and KH can also be employed in DMF and DMSO at room temperature or at a higher temperature. Alkylation sometimes yields regioisomers when more than one nitrogen atom is present in the heterocycle. These isomers can be separated by standard methods such as crystallization or chromatography. Once alkylated, the Y group can be coupled to the boronic acid moiety and all protecting groups removed to yield compounds of Formula I by procedures described previously.

Compounds where R¹ =1,2,4-triazole can be prepared by the route of H. Paul, G. Hilgetag and G. Jahnchen, Chem. Ber., 101, 2033 (1968) which is depicted in Scheme 18. Imidate ester 92 is formed from nitrile 91 by the method of P. Keynaud and R. D. Moreau Bull. Soc. Chim. France, 2997 (1964). Hydrazide 99 is easily ##STR45## prepared via the action of hydrazine on the corresponding methyl ester precursor. It is understood that R¹³ of 91 and 94 do not necessarily have to be in their final form, for example. In each case, they can exist as either a protected species or in the form of a precursor to R¹³.

Alkylation of triazole 96 yields two isomeric products 97 and 98 when the R¹³ groups are not identical. These intermediates can be converted into final products in the usual fashion as shown in Scheme 19. ##STR46##

The regioselective syntheses of both 97 and 98 are shown in Scheme 20. Imidate ester 93 is reacted with hydrazine to form amidrazone 103. Alkylation with methyl μ-bromoacetate yields 194. Ring closure with either an ortho-ester, acid chloride or anhydride yields triazole 98. For a similar triazole synthesis, see David B. Reitz, European Patent Application 508, 445, published 14.10.92., G. D. Searle & Co. For schemes 20, and 22, the different R¹³ groups are differentiated from one another by the placement of a prime symbol next to one of the R¹³ groups, i.e. R^(13'). ##STR47##

Yet another regioselective synthesis of 97 or 98 is depicted in Scheme 21 following a similar sequence as was shown in Scheme 20 (D. B. Reitz, ibid.). ##STR48##

1,2,4-Triazoles also undergo selective metalation at the 5-position when the nitrogen at the 1-position is suitably protected. The metallated triazole can then be quenched through the addition of an electrophile to result in a newly functionalized triazole at the 5-position. Suitable protecting groups are benzyl and trityl. (D. K. Anderson, et al., J. Heterocyclic Chem., 23, 1257 (1986) as well as diethoxymethyl (S. Ohta, et al., Chem. Pharm. Bull., 41, 1226 (1993). The 3-position can also be metallated if the 5-position is suitably protected (S. Ohta et al., ibid.). Thus here we have two other methods for introducing R¹³ substituents at the 5- or 3-positions of the 1,2,4-triazoles.

Compounds where R¹ =1,2,3-triazole can be synthesized via the 1,3-dipolar cycloaddition of an azide to an alkyne as shown in Scheme 22 (for an example of this cycloaddition reaction, see W. Kirmse and L. Horner Justus Liebigs Ann. Chem. (1958) 614, 1). ##STR49##

Compounds where R¹ =tetrazole can be synthesized by the methods outlined in Scheme 23. In line a, three methods are given for the conversion of a nitrile into a tetrazole (ammonium chloride/sodium azide: W. G. Finnegan et al., J. Am. Chem. Soc. 1958, 80, 3908; trialkyltin azides: J. G. Luitjen et al., Rec. Tray. Chim. Pays-Bas; dialkyltin oxide: S. Wittenberger and B. G. Donner, J. Org. Chem., 1993, 58, 4139).

In Scheme 23, line b, two procedures are given for the regioselective synthesis of 1,5-disubstituted tetrazoles (DEAD, Ph₃ P, TMSN₃ : J. V. Duncia, M. E. Pierce, J. B. Santella III, J. Org. Chem. 1991, 56 2395; Tf₂ O/NaN₃ : E. W. Thomas Synthesis, 1993, 767) which can be more difficult to synthesize due to the steric crowding of the substituents.

Compounds where R¹ is an oxazole may be synthesized by a variety of methods including those outlined in Scheme 24. The oldest synthesis and one of the most versatile is shown on line a), namely the cyclodehydration of 2-acylaminoketones (The Robinson-Gabriel Synthesis) (see I. J. Turchi in Oxazoles, Turchi, I. J., ed. John Wiley and Sons, New York (1986) p. 1). The 2-acylaminoketone starting materials may be synthesized from the Dakin-West reaction and modifications thereof (G. H. Cleland and F. S. Bennett Synthesis (1985)₆₈₁ and references therein). Some cyclodehydration agents include PCl₅, H₂ SO₄, P₂ O₅, SOCl₂, etc). ##STR50##

R^(a), R^(b) and R^(c) are equal to R¹³ which is described in the scope of this application. R¹³ in Scheme 24 does not have to be in finalized form as it appears in the scope, but can be in protected form or in the form of suitable precursors. It is understood that only when the entire molecule of formula I is synthesized do all of the substituents have to appear in their final forms as stated in the scope. Protected forms and suitable precursors to R¹³ are readily recognized by one skilled in the art of organic synthesis.

In line b, the reaction of α-acylketones 131 with ammonium acetate/acetic acid also yields oxazole 130 (D. Davidson, M. Weiss, M. Jelling J. Org. Chem. (1937), 328). In line c, we find the regioselective formation of oxazole 130 from the reaction of an α-haloketone 134 with amide 133 (R. Lakham, B. Ternai, Adv, Heterocycl. Chem. (1974) 17, 99; I. J. Turchi, M. J. S. Dewar, Chem. Rev. (1975), 75, 389). Acid chlorides 135 react with oximes 136 to yield after a 3,3! sigmatropic rearrangement (138) oxazole 130 as shown in line d (G. S. Reddy and M. V. Bhatt Ind. J. Chem. (1981) 208, 322; M. V. Bhatt, G. S. Reddy Tet. Lett. (1980) 21, 2359). In line e, μ-azidoketones (140), after reaction with triphenylphosphine to yield 141, react with acid chloride 135 to yield oxazole 130 (E. Zbiral, E. Bauer, J. Stroh Monatsh. Chem. (1971) 102, 168). Finally, oxazoles undergo deprotonation with strong bases such as n-BuLi at the 2-position when the 4 and 5 positions are blocked and after quenching with an electrophile can yield oxazole 130 (R. Schroder, V. Schollkopf, E. Blume, I. Hoppe Liebigs Ann. Chem., (1975) 533). As stated earlier, R¹³ can be either in final form as defined in the scope of this application or in the form of precursor functionality which later on can be elaborated into final form by methods familiar to one skilled in the art. This holds true not only for the oxazoles discussed here, but for all of the other heterocyclic systems in this application where R¹³ appears as substituents.

Oxazoles are most readily brominated at the 5-position followed by the 4-position and finally the 2-position. A brominated oxazole (as well as other brominated heterocycles in this application) can undergo aryl cross-coupling reactions catalyzed by transition metals to yield aryl-or heteroaryl-substituted oxazoles (See for example E.-I. Negishi; A. O. King; N. Okukado J. Org. Chem. (1977) 42, 1821).

Compounds where R¹ is an isoxazole may be synthesized by the methods outlined in Scheme 25. In line a, reaction of 1,3-diketone 143with hydroxylamine yields oxazoles 144 and 145. Nitrile oxide 146 can also add across the triple bond of alkyne 147 to yield isoxazoles 144 and 145. (See P. Grunanger and P. Vita-Finsi Isoxazoles, v. 49 pt. 1 of The Chemistry of Heterocyclic Compounds, E. C. Taylor and A. Weissberger, eds., John Wiley and Sons (New York: 1991) p. 126). ##STR51##

As discussed previously R^(a), R^(b) and R^(c) in Scheme 25 are again equal to R¹³ and are not necessarily in final form as they appear in the scope of this application.

Compounds wherein R¹ is a thiazole may be synthesized by the method depicted in Scheme 26, which mimics the route of Scheme 24c) describing a route for oxazoles. Thus thioamide 148 reacts with α-halocarbonyl compound 134 to yield thiazole 149. Again as for the oxazole, R^(a), R^(b), and R^(c) have the same definitions. For the synthesis of thiazoles, by the route depicted in Scheme 26, see G. Vernin "General Synthetic Methods for Thiazole and Thiazolium Salts" in Thiazole and Its Derivatives, J. V. Metzger, ed., volume 34, pt. 1 in The Chemistry of Heterocyclic Compounds, A. Weissberger and E. C. Taylor, eds. John Wiley and Sons (New York:1979) p. 180. ##STR52##

Compounds wherein R¹ is a 1,2,5-thiadiazole may be synthesized by the methods shown in Scheme 27. Diamine 150 may be reacted with sulfur monochloride to yield 1,2,5-thiadiazole 151. Likewise, α-diketone 152 may be converted into bisoxime 153 which also reacts with S₂ Cl₂ to yield 151 (L. M. Weinstock, P. Davis, B. Handelsman, R. Tull J. Org. Chem. (1967) 32, 2823). Z is defined in Scheme 24. ##STR53##

Compounds wherein R¹ is a 1,2,4-thiadiazole may be synthesized by the method depicted in Scheme 28. Oxidation of thioamide 154 with hydrogen peroxide yields S-oxide 155 which must be stored at 0° C. Further reaction of the S-oxide intermediate with thioamide 156 yields thioacylamidine 157 which cyclizes to product 158 (V. Goerdeler, H. Porrmann Chem. Ber. (1962) 95, 627). R^(a) and R^(b) are as defined previously in Scheme 24.

Compounds where R¹ is a furan may be synthesized by the methods shown in Scheme 29, but as understood by one skilled in the art, not limited thereto, as in the case as for all of the schemes in this patent application. In line a, cyclodehydration of 1,4-dicarbonyl compound 159 yields furan 160 (L. D. Krasnoslobodskaya, Ya. L Gol'dfarb Russ. Chem. Rev. (Engl. Trans.) 1969, 38, 389). In line b, α-bromoketone or aldehyde 161 protected as its dimethyl ketal or acetal reacts with trimethylsilylenol ether 162 to yield intermediate 163 which cyclizes to furan 160 (T. Mukaiyama, H. Ishihara, K. Inomata Chem. Lett., 1975, 527). R^(a), R^(b), R^(c), and R^(d) are R¹³ which is described in the scope of this application and with similar limitations as were described under Scheme 24 for R¹³ with regards to being in final form or not.

Compounds where R¹ is a thiophene may be synthesized by the methods shown in Scheme 30. In line a, 1,4-dicarbonyl compound 159 is reacted with a phosphorous sulfide (phosphorous pentasullfide, phosphorous trisulfide, phosphorous heptasulfide, etc.) to yield thiophene 164 (H. D. Hartough, Chem. Heterocycl. Compd., 1952, 3, 1). The dicarbonyl compound 159 also reacts with H₂ S to favor thiophenes at lower temperatures (-50° C.) (F. Duus Tetrahedron, 1976, 32, 2817). Reaction of alkenes 165 or 166 (line b) with sulfur and heat also yield thiophene 16 (A. S. Broun, M. G. Voronkov J. Gen. Chem. USSR, (Engl. Trans.) (1947) 17, 1162; M. g. Voronkov, A. S. Broun, ibid, (1948) 18, 700; J. Schmitt., M. Suquet, R. Fallard (C. R. Hebd, Seances Acad, Sci. (1956) 242, 1738. R^(a), R^(b), R^(c) and R^(d) are as defined in Scheme 29. ##STR54##

Compounds where R¹ is a pyridine may be synthesized by the methods shown in Scheme 31. It is to be understood that each scheme and each reaction has its own scope and limitations and that no one synthesis is universally applicable. It is also to be understood that one skilled in the art will be able to determine which synthesis is best suited for his or her needs. In line a, reaction of enamine 167 with ethynyl ketone 168 will cyclize to pyridine 170 (F. Bohlmann, D. Rahtz Chem. Ber. (1957)90, 2265). Enamino ketones 171 (line b) condense with 1,3-diketones or beta-keto esters 172 to yield pyridine 174 where R is alkyl, aryl or alkoxy and aryloxy (N. K. Kachetkov, A. Gonsales, A. Nesmeyanov Dokl. Akad, Navk, SSSR (1951) 79, 609; S. Auricchio, R. Bernardi, A. Ricca Tet. Lett. (1976) 9831; H. Henecka Chem. Ber. (1949) 82, 41).

The Hantsch dihydropyridine synthesis can be used in the synthesis of pyridines as shown in line c. There are many modifications of this synthesis of which only one is shown. Reaction of 175 with beta-aminocrotonate 176 yields dihydropyridine 177 (F. Bassett, H. Meyer, E. Wehinger Angew. Chem. Int. Ed. Engl. (1981) 20, 762). Further oxidation with, for example, dilute nitric acid yields pyridine 178 where R and R¹ can be different alkoxy groups (E. Knoevenagel, W. Rushhaupt Ber. (1898) 31 1025). Cycloaddition of oxazole 179 with alkene 180 can also yield a pyridine (182) (M. Ya Karpeiskii, V. L. Florent'ev Russ. Chem. Rev. (Engl. Trans.) (1969) 38, 540; R. Lakhan, B. Ternai Adv. Heterocyl. Chem. (1974) 17, 99). In all of these pyridine synthesis, R^(a), R^(b), R^(c), and R^(d) are as described for Scheme 29. All of the substituents around the pyridine ring can be in final form or in the form of a precursor to a given functional group as would be recognized by one skilled in the art. Finally, in line e, hydroxypyridines, such as 183, may be triflated and coupled with an aryl-or heteroarylboronic acid or aryl-or heteroaryltrialkylstannane using a transition metal catalyst such as Pd to yield aryl or heteroarylpyridinecarboxylic acids, such as 186. This in turn may be coupled to aminoboronic acid esters as discussed previously to yield compounds of Formula I. Halogens, such as Br or I may be used instead of triflate in compound 184 to undergo what is known as the Suzuki coupling reaction. R and R^(1') in line e) are any of the allowed phenyl substituents in the scope of this application (Suzuki reactions: A. Suzuki Pure Appl. Chem. (1985) 57, 1749). ##STR55##

Compounds where R¹ is a pyridazine may be synthesized by the routes shown in Scheme 32. Reaction of 1,4-carbonyl compound 187 with hydrazine yields pyridazine 188. If the 1,4-dicarbonyl compound is saturated as in line b (compound159), then the product from the reaction with hydrazine 189must be oxidized to yield pyridazine 188 (K. C. Nicolaou, W. E. Barnette, R. L. Magolda J. Am. Chem. Soc. (1979) 101, 766; ##STR56## M. Tisler, B. Stanovnik "Pyridazines and their Benzo Derivatives" in A. R. Katrizky, C W. Rees Comprehensive Heterocyclic Chemistry, v.3 (Pergamon Press: Oxford), 1984, p. 45). Halopyridazines or hydroxypyridazines may also undergo the same aromatic cross-coupling reactions as were described for pyridines. R^(a), R^(b), R^(c) and R^(d), etc., are defined the same as in the pyridine case.

Compounds wherein R¹ is a pyrimidine may be synthesized by the methods shown in Scheme 33. Reaction of 1,3-dicarbonyl compound 190 with amidine 191 yields pyrimidine 192 (D. J. Brown, S. F. Mason The Pyrimidines in A. Weissberger ed. The Chemistry of Heterocyclic Compounds, (John Wiley: New York) 1962, p. 31). ##STR57## Reaction of amidine 191 with 193 also yields pyrimidines (P. Schenone, L. Sansebastiano, L. Mosti J. Heterocyclic Chem. (1990) 27, 295). R^(a), R^(b), R^(c), and R^(d) are as defined previously in Scheme 32. Halopyrimidines or hydroxypyrimidines may also undergo the same aromatic cross-coupling reactions as were described for pyridines. ##STR58##

Compounds in which R¹ is a 1,2,4-triazine my be synthesized by the procedures outlined in Scheme 34. In line a, 1,3-dicarbonyl compound 194 is condensed with amidrazone 195 to yield triazine 196 (H. Neunhoeffer and P. F. Wiley Chemisrty of 1,2,3-Triazines and 1,2,4-Triazines and Pentazines, v. 33 in A. Weissberger, E. C. Taylor, eds., The Chemistry of Hetrocyclic Compounds John Wiley and Sons (New York: 1978) pp 194-200 and p. 524). In line b, cyclization of acylhydrazone 197 with ammonia or ammonium acetate leads to triazine 196 (H. Neunhoeffer, P. F. Wiley, ibid., p. 196, 197). In line c, reaction 1,2-dicarbonyl compound 194 with oxalamidrazonates 198 yields 1,2,4-triazine ester 199. Saponification of 199 yields 200 which can be decarboxylated to yield 1,2,4-triazine 201 (H. Neunhoeffer, P. F. Wiley, ibid., p. 526). R^(a), R^(b), and R^(c) are as defined in the pyridine case. Halotriazines or hydroxytriazines may undergo the same aromatic cross-coupling reactions as were described earlier for pyridines.

Compounds in which R¹ is as described in lines k and l in the scope of this application may be synthesized by the methods described in Scheme 35. If heterocycle --J--K--L--M--Q-- 202 contains a bromine, iodine or a hydroxyl group (which can be triflated) designated by X, then it can undergo a Suzuki coupling to yield 204 where u is 0 (A. Suzuki, ibid) (Scheme 35, line a). If instead of B(OH)₂ a trialkyltin group is present, then a Stille coupling can be performed when X=triflate (J. K. Stille Angew. Chem. Int. Ed. Engl. (1986) 25 508; J. K. Stille Pure Appl. Chem. (1985) 57, 1771). ##STR59## The X and B(OH)₂ (or trialkyltin) moieties may be reversed so that now X=B(OH)₂ (or R₃ Sn) and the phenyl of 203 contains halogen or triflate group. The same coupling procedures may be used in synthesizing compounds where R¹ is described by line 1 and u is 0 as were used in synthesizing compounds where R¹ is described by line k and u is 0.

When u is not 0, heterocycle 205 and its six-membered ring counterpart --C--W--R--T--U--V-- (described in line 1) must be synthesized from scratch by the methods described heretofore, with the --(CH₂)_(u) -Phenyl--(CH₂)_(m) CO₂ R group being one of the substituents in final or precursor form. If heterocycle 205 contains an N--H which is alkylatable, then alkylation with 206 where X is Cl, Br, I, mesylate tosylate or triflate yields 207 (Scheme 35, line b). The esters 204 and 297 can then be hydrolyzed to the free acid and coupled with aminoboronic acid ester derivative as described in Scheme 4, for example, to yield boronic acid esters which can also be hydrolyzed to the corresponding free boronic acid products.

A general method (Scheme 36) for the synthesis of 4-carboxydihydroheterocycles (oxazolines, thiazolines, imidazolines) utilizes the condensation of an α-amino acid ester (210) with an imidate (211) to provide 212, see: Meyers, A. I.; Hanagan, M. A.; Mazzu, A. L. Heterocycles 1981, 15, 361; Meyers, A. I.; Whitten, C. E. Heterocycles 1976, 1, 1687; North, M.; Pattenden, G. Tetrahedron 1990, 46, 8267; Jones, R. C. F.; Ward, G. J. Tetrahedron Lett. 1988, 29, 3853. In the case where R²⁰ =H, the cyclization might be conducted with trimethyl orthoformate instead of 211, see: Martin, P. K. et al. J. Org. Chem. 1968, 33, 3758. For compounds that are substituted only at the 2-position of the heterocycle, serine or cysteine might be used as the amino acid ester partner. The dihydroimidazole-based materials would be prepared from an N.sup.α -monoprotected diaminopropionic acid to prevent tautomerization of the double bond once the cyclic system of 212 has been formed, see: Martin, P. K. et al. J. Org. Chem. 1968, 33, 3758. Hydrolysis of the ester then affords carboxylic acid 213. ##STR60##

It may be desirable to prepare more highly substituted heterocycles as well (Scheme 37). An approach to the oxazoline class could utilize reaction between the anion of 215 and formaldehyde to provide adducts 216 as recorded by Kanemasa, S. et al. Tetrahedron Lett. 1993, 34, 677 and Ito, Y. et al. Tetrahedron 1988, 44, 5253. Hydrolysis of the imine should deliver 217, an example of an G-substituted α-amino acids, as a mixture of isomers. Condensation as before with imidate (211) should generate cyclic moieties of general structure 218 which are hydrolyzed to 219.

The corresponding thiazolines should be available by installing a sulfhydryl group prior to cyclocondensation. To that end, N--protection of 217, followed by reaction with a sulfur nucleophile, a thiol ester or an inorganic salt thereof, based on the work reported by Mitsunobu, O. Synthesis 1981, 1, and Yuan, W. et al. J. Med. Chem. 1993, 36, 211, should provide the substituted cysteine (220) upon premoval of the N-protecting group. Subsequent reaction with the imidate should deliver 221 and ultimately 222, after hydrolysis of the ester. ##STR61##

The imidazolines should be obtained via the condensation described by Jones, R. C. F.; Ward, G. J. Tetrahedron Lett. 1988, 29, 3853, of a suitable diamino acid with imidate 211. The preparation parallels the sequences discussed above where the anion of 215 would be expected to generate adduct 223 as described by Gilbert, I. et al. Tetrahedron Lett. 1991, 32, 2277. Manipulation of the protecting groups and implementation of the aforementioned cyclization should give imidazoline 225 which may be converted to the corresponding carboxylic acid 226.

Using an analogous synthetic sequence (Scheme 38), the polysubstituted versions of these heterocycles should also be accessible. For the oxazo--or imidazo--type compounds, reaction of the anion of 215 with an electrophile 227 should deliver 228, as reported by Kanemasa, S. et al. Tetrahedron Lett. 1993, 34, 677 cf. Meyer, R. et al. Liebigs Ann. Chem. 1977, 1183!, and liberation of the a -amino group should then provide 229, as a mixture of isomers. Application of the now standard cyclocondensation should complete the synthesis of 231 upon hydrolysis of 230.

A similar sequence should provide an entry into the thiazolines series (235). However, in the case where R^(3b) =H, this material would be prepared by converting 232 to the corresponding mercaptan 233 using the conditions described earlier; the ester in 234 could then be hydrolyzed to afford 235. This reaction sequence would be preferred to avoid use of a presumably unstable thioaldehyde (227 where U=S and R^(3b) =H), see: Takahashi, T. et al. Heterocycles 1993, 36, 1601 and references therein. ##STR62##

Alternative methods for the preparation of these polysubstitutued heterocycles employ (Scheme 39) the addition of the anion of isocyanide 236 to an electrophile 227 to provide the heterocycle 237, see: Ito, Y. et al. Tetrahedron Lett. 1989, 30, 4681; Ito, Y. et al. Tetrahedron Lett. 1988, 29, 6321, 235; Ito, Y. et al. Tetrahedron Lett. 1987, 28, 6215; Ito, Y. et al. Tetrahedron 1988, 44, 5253; Meyer, R. et al. Liebigs Ann. Chem. 1977, 1183. The carboxylic ester may be manipulated at this time, however the preferred sequence would implement either an exchange reaction mediated by a transition metal catalyst as reported by Ito, Y. et al. Tetrahedron 1988, 44, 5253 to provide derivatives 238; standard hydrolysis followed by reaction with imidate 211 would also yield 238. Subsequent conversion to the carboxylic acid 239 should proceed smoothly. For cyclic compounds (243) where R²⁰ =H, the preferred sequence would involve the sequential hydrolysis of adduct 240, transformation of the hydroxyl group into a sulfhydryl function, cyclocondensation to thiazoline 242 and finally hydrolysis to afford the desired carboxylic acid 243. ##STR63##

Another noteworthy method (Scheme 40) for the assembly of oxazolines and thiazolines utilizes an appropriate N-acyl-β-hydroxy-α-amino acid (244) which reacts intramolecularly by cyclization of the amide carbonyl onto the hydroxyl group of the amino acid. This transformation may occur upon treatment with triphenylphosphine and an azodicarboxylate, as reported by Wipf, P.; Miller, C. P. Tetrahedron Lett. 1992, 33, 6267, 907 and Galeotti, N. et al. Ibid., 2807, or through the use of diphenyl sulfoxide and triflic anhydride, as demonstrated by Yokokawa, F. et al. Synlett 1992, 153, to generate the requisite ring system; in 245. Hydrolysis of the ester then provides 246. Alternatively, this cyclization may be effected by intramolecular displacement of the corresponding halo derivative (--OH→halogen in 244), which is generated in situ, to provide the oxazoline (245), see: Evans, D. A. et al. J. Org. Chem. 1992, 57, 1961. ##STR64##

The regioisomeric 5-carboxyheterocycles may be synthesized (Scheme 41) by condensation of an appropriate α-functionalized β-amino acid with imidate 211; for an example of this type of cyclization, see: Wolfe, S. et al. Tetrahedron Lett. 1979, 3913. In the event, nucleophilic opening of an a, b-epoxy acid (247) with an inorganic azide such as lithium azide according to Chong, J. M.; Sharpless, K. B. J. Org. Chem. 1985, 50, 1563 should provide 248; the corresponding esters also participate in this reaction, see: Commerçon, A. et al. Tetrahedron Lett. 1992, 33, 5185. Reduction should give the requisite (α-hydroxy-β-amino acid 249. Alternatively, it may be desirable to prepare 249 from an a--amino acid directly as described by Poss, M. A.; Reid J. A. Tetrahedron Lett. 1992, 33, 1411, by reaction of the appropriate N-BOC compound (250) with 2-furyllithium to provide vicinal amino alcohol (251); manipulation of the furan moiety and deprotection then generates 249. A similar approach using 2-ithiothiazoles may also be useful, see: Dondoni, A.; Perrone, D. Tetrahedron Lett. 1992, 33, 7259. ##STR65##

Completion of the syntheses of the heterocycles should follow precedent. Reaction with of 249 with 211 should provide oxazoline 254 directly. This alcohol may also be used in a sequence described previously to allow for incorporartion of sulfur and ultimately provide 250; this mercaptan should lead to thiazoline 251. Additionally, 249 could be employed as a substrate for reaction with a nitrogen based nucleophile, see: Mitsunobu, O. Synthesis 1981, 1 cf. Cardani, S. et al. Tetrahedron 1988, 44, 5563!, to deliver 252 as a precursor for imidazoline 253.

The regioisomeric imiodazolines should be available from other routes as well (Scheme 42). One method would call for hydrolysis of imine 223, discussed earlier in Scheme 37, followed by protection of the newly liberated α-amino group to give 254. Cleavage of the phthaloyl residue and reaction with imidate 211 should provide 255 which is hydrolyzed to 256. An alternative approach calls for reaction of an α-bromo-α,β-unsaturated ester (257) with an amidine (258) sterically hindered (P is large ) materials do not react!to generate 259 in a single step as reported by Marsura, A. et al. Synthesis 1985, 537; hydrolysis of the ester should yield the acid 260. ##STR66##

The several types of inhibitors disclosed in this invention can be broadly classified by their electrophilic functional group A, as defined in Formula (I). The compounds described below, unlike the boron containing peptides, utilize a highly electrophilic carbon atom at A to interact with the active site serine of thrombin. The precursor for the electrophilic carbon inhibitors is the appropriately protected amino acid (261) of Scheme 43. ##STR67## The preparation of (261) can be found in the general chemical literature, one such reference being the review by Morrison and Mosher (1976). According to Scheme 43 various terminal functional groups are available from (261): the formamidino-(262), cyanoguanidino-(263), hydroxyguanidino-(264) and guanidino-analogs (265).

The preparation of amidine derivative (267) and phenylguanidines of formula (269) from amino acids (266) and (268), respectively, is shown in Scheme 44. The conditions used Lo prepare amidines of formula (267) is discussed for (303) of Scheme 53 while the method for formamidinylation of (268) to give (269) is the same as that described to prepare (295) of Scheme 52. ##STR68##

As shown in Scheme 45, appropriately protected derivatives of formulae (261-269), wherein M is an alkyl or benzyl group can be coupled with N,N-disubstituted acid (270) or (271) (wherein M is hydrogen). The X group in compounds of formulae (261) through (269) and (272) in Scheme 45, as well as in compounds illustrated in the Schemes to follow, is a protected version of the terminal functional group X, as defined by Formula (I), unless deprotection is indicated to obtain the final compound of the sequence. ##STR69## It is understood that the protecting group(s) used should compatible with the conditions of the process discussed; a good source for information on protecting group chemistry is Greene and Wuts (1991).

The preparation of the thrombin inhibitors trihalomethyl ketone (274) and α-ketoester (275) are shown in Scheme 46. The coupled ester (272), wherein M is alkyl or benzyl can be converted to the acid (M is hydrogen) by the methodology appropriate for the particular ester functionality as described in Greene and Wuts (1984). The aldehyde (273) can be prepared by selective reduction of the acid (272, M is hydrogen) to the primary alcohol followed by oxidation. ##STR70## To obtain the primary alcohol, the acid can be transformed to the mixed anhydride by condensation of the trialkylammonium salt of the acid with an alkyl- or arylchloroformate in an inert non-polar solvent such as tetrahydrofuran, 1,2-dimethoxyethane or toluene at -78° C. to room temperature. The solution of the resulting mixed anhydride is filtered and reduced to the peptidyl alcohol with an excess of a borohydride reducing agent in a compatible solvent like water or an alcohol at -78° C. to room temperature according to the method of Rodriguez et. al., Tetrahedron Lett. 32, 923 (1991). The peptidyl alcohol can be oxidized to aldehyde (273) without over oxidation by a variety of procedures, as detailed by Hudlicky in Oxidations in Organic Chemistry, American Chemical Society, p. 114 (1991); the preferred methods include Swern oxidation described by Omura and Swern, Tetrahedron 34, 1651 (1978); and the Pfitzner-Moffat oxidation described by Fearon et al. in J. Med. Chem. 30, 1617 (1987). A two step protocol reported by Edwards, Tetrahedron Lett. 33, 4279 (1992) can be used to prepare the trifluoromethyl ketones (274) (J is fluorine) from aldehyde (273). In this procedure a metallated trifluoromethyl anion is generated from an excess of trifluoromethyliodide or -bromide and an active metal such as zinc, magnesium, lithium or cadmium in inert, anhydrous solvents like tetrahydrofuran or N,N-dimethylformamide at temperatures of -100° C. up to the reflux point of the solvent. Alternatively, the metallated trifluoromethyl anion may be generated by the transmetallation of trifluoromethyliodide or -bromide with an organometallic compound such as a Grignard reagent or alkyllithium compound in an inert solvent like tetrahydrofuran, hexane or ether at temperatures ranging from -78° C. up to the reflux point of the selected solvent. Aldehyde (273) can be added to the solution of the metallated trifluoromethyl anion to form the trifluoroethanol derivative at temperatures of -100° C. or higher. To obtain the trifluoromethyl ketone (274) where J is fluoro, the alcohol is oxidized by the Pfitzner-Moffat or Swern procedure. Removal of the protecting group(s) on terminal group X by the appropriate method will provide the thrombin inhibitors of formulae (274).

Trihalomethyl analogs of (274), where J is fluoro can also be prepared from aldehyde (273) by a different method. The trihalomethyl ketones are prepared by treating aldehyde (273) with either the trimethylsilyl trihaloacetate or the potassium or sodium trihaloacetate in a polar solvent such as an alcohol, N,N-dimethylformamide or methylsulfoxide with or without a base such as a trialkyl amine, potassium carbonate or sodium hydroxide at temperatures of -78° C. or higher according to the method of Beaulieu, Tetrahedron Lett. 32, 1031 (1991); Shell Int. Res., European Patent Application EP 16504). The resulting α,α,α-trihaloethanol is oxidized and group X can be deprotected as above to give the thrombin inhibitors or formulae (274).

The α-ketoester thrombin inhibitors, exemplified by (276), are prepared according to a route disclosed by Iwanowicz et. al. in Bioorgan. Med. Chem. Lett. 12, 1607 (1992). The tris(ethylthio)methyl anion is added to the peptidyl aldehyde (273) in a solvent such as tetrahydrofuran, 1,2-dimethoxyethane or toluene at -100° C. or higher to give the alcohol (275). The α-hydroxyl ester is generated from (275) by treatment with a mixture of mercuric salts, such as mercuric chloride and mercuric oxide, in an alcohol or water. Swern or Pfitzner-Moffat oxidation of the s-hydroxyl ester followed by the deprotection of substituent X protecting group provides thrombin inhibitors of formula (276).

Another method for the preparation of compound (276) substitutes a 1-lithio-1-alkoxyethene or 1-magnesio-1-alkoxyethene for the tris(ethylthio)methyl anion of Scheme 15 in an addition reaction with peptidyl aldehyde (273). There can be obtained an adduct analogus to the tris(ethylthio)hydroxyethyl compound (275) when excess 1-magnesio- or 1-lithio-1-alkoxyethene anion is stirred at temperatures ranging from -100° C. to ambient temperature with (273) in anhydrous solvents such as diethyl ether or tetrahydrofuran. This alkoxyolefin product may then be transformed to (276) by oxidative cleavage with reagents such as ozone or periodate in an inert solvent such as a halohydrocarbon, lower alkyl ketone, an alcohol or water at temperatures ranging from -100° C. to ambient temperature, followed by oxidation of the intervening α-hydroxyester and deprotection as described above.

The preparation of the α,α-dihalomethylketone thrombin inhibitors of this invention is outlined in Scheme 47. ##STR71## The α,α-dihalomethylketone (279), where J is fluoro can be prepared from the aldehyde (273) by selective reaction of the aldehyde with the anion of the corresponding dihalomethane. The metallated dihalomethane anion is generated from one equivalent each of a strong hindered base, such as lithium tetramethylpiperidide or tertbutyllithium, and the selected dihalomethane in an anhydrous, inert solvent like tetrahydrofuran or 1,2-dimethoxyethane at -100° C. or higher according to the method of Taguchi et. al. Bull. Chem. Soc. Jpn., 50, 1588 (1977). The metallated dihalomethane anion can be added to the aldehyde (273) at -100° C. or higher. Alternatively, the dihalomethane anion is generated from a dihalomethyl(trimethyl)silane and an anhydrous fluoride ion source such as tris(diethylamino)sulfonium difluoromethyl silicate in an inert solvent like benzene, acetonitrile or tetrahydrofuran at -78° C. or higher, then (273) can be added to give dihaloethanol (278) according to the method of Fujita and Hiyama, J. Am. Chem. Soc. 107, 4085 (1985). The resulting dihaloethanol can be oxidized to ketone (279) by the Swern or Pfitzner-Moffat procedure. Removal of the protecting group(s) on substituent X of (279) gives the α,α-dihalomethylketone thrombin inhibitors.

α-Halomethylketone thrombin inhibitors can be prepared by the process illustrated in Scheme 48. The acid chloride (281) can be prepared from acid (272), wherein M is hydrogen or its trialkylammonium, sodium or potassium salt with a chlorinating agent such as thionyl chloride, oxalyl chloride or dichloromethylmethyl ether in a solvent like tetrahydrofuran or dichloromethane with or without a catalytic amount of N,N-dimethylformamide at -78° C. or higher. Alternatively, the mixed anhydride of (272)_(m) ay be prepared as described for (272) in Scheme 46. Compound (281) or the mixed anhydride of (272) can be treated with an ether solution of diazomethane and either anhydrous hydrogen fluoride or hydrogen chloride gas according to that described by McPhee and Klingsbury, Org. Synth. Coll. III, 119 (1955); or hydrogen bromide according to the method Miescher and Kaji, Helv. Chim. Acta. 24, 1471 (1941). ##STR72## Selection of the hydrogen fluoride gas will give the α-fluoromethylketone analog, (282) wherein J is fluoro; and hydrogen chloride gas gives the α-chloromethylketone analog (282) wherein J is chloro. Deprotection of X gives the corresponding thrombin inhibitors of (282).

The general preparative route for the α,β-diketoester, -amide and -ketone thrombin inhibitors of this invention is exemplified in Scheme 49. Compound (281) or the mixed anhydride of (272) can be reacted with a Wittig reagent such as methyl (triphenyl-phosphoranylidene)acetate in a solvent like tetrahydrofuran or acetonitrile at temperatures ranging from 0° C. to the reflux point of the solvent to give (284). Oxidative cleavage of the phosphoranylidene (284) with an oxidizing agent like ozone or OXONE™ in an inert solvent such as tetrahydrofuran, dichloromethane or water at temperatures of -78° C. or higher gives the vicinal tricarbonyl compound (285), analogous to that described by Wasserman and Vu, Tetrahedron Lett. 31, 5205 (1990). Cleavage of the protecting group can provide thrombin inhibitors of formula (285). ##STR73##

The preparative routes for the synthesis of the α-mono- and α,α-dihalo-β-ketoester -amide and ketone thrombin inhibitors of this invention are summarized in Scheme 50. The exemplified β-ketoester (287) is available from the acid derivative (272). The acid (272) can be treated with carbonyl diimidazole in an inert solvent such as tetrahydrofuran or dichloromethane at 0° C. or higher to form the acyl imidazole. This acyl imidazole, or the mixed anhydride of (272), can be further reacted with lithioethylacetate in solvents such as 1,2-dimethoxyethane or tetrahydrofuran/hexane at temperatures ranging from -100° C. to ambient temperature, according to the method of Dow, J. Org. Chem. 55, 386 (1990) to give β-ketoester (287). ##STR74## Compound (287) serves as a substrate for both mono- and dihalogenation. The α-monochloro analog of (288), where J is each chlorine and hydrogen, can be prepared by controlled halogenation reactions with reagents like N-chlorosuccinimide or thionyl chloride in an inert halogenated solvent and at temperatures ranging from -20° C. to the reflux point of the selected solvent according to the methods of Uhle, J. Am. Chem. Soc. 83, 1460 (1961); and DeKimpe et. al., Synthesis 2, 188 (1987). The α,α-dihalo analog (289) where J is chloro is available from halogenation with molecular chlorine in a halogenated solvent at temperatures of -20° C. or higher according to the method of Bigelow and Hanslick, Org. Syn. Coll. II, 244 (1943). Reagents such as N-fluorobis (trifluoromethyl sulfonyl!imide are useful for the preparation of mono- and difluoro analogs (288) and (289) by reacting the appropriate stoichiometry of this reagent with (287) in a halogenated solvent at temperatures of -78° C. or higher according to the method of Resnati and DesMarteau, J. Org. Chem. 56, 4925 (1991). Deprotection of substituent X of the halogenation products (288) and (289) can provide the corresponding thrombin inhibitors.

Compounds of formula (287) also serves as a substrate for the preparation of tricarbonyl derivatives such as (285) (Scheme 49). Condensation of (287) with an aldehyde, such as benzaldehyde, gives an β-ene-α,γdione. This ene-dione can be oxidatively cleaved with reagents like ozone or periodate to give tricarbonyl analog (285).

The preparation of the mono- and dihalomethylketone thrombin inhibitors is outlined in Scheme 51. The intermediates formed in the preparation of the α-mono- and α,α-dihalo-β-ketoester thrombin inhibitors of Scheme 49 can be used in these preparations. ##STR75## The decarboxylation of these halogenation products, (288) and (289), can be effected by saponification of the ester with mild aqueous base such as potassium carbonate or sodium hydroxide in water miscible solvents like an alcohol, tetrahydrofuran or N,N-dimethylformamide, followed by adjusting the pH to a range of 4 to 6. This mixture can be either stirred at ambient temperatures or heated at various temperatures up to the reflux point of the solvent chosen until the formation of (279) or (282) is complete and is similar to that reported in Matsuda et. al., Tetrahedron Lett. 30, 4259 (1989). Removal of protecting group(s) can provide thrombin inhibitors corresponding to (279) or (282).

A process for the preparation of the boropeptide thrombin inhibitors of this invention from intermediates (291) and (292) is disclosed in Scheme 52. Compound (291) serves as a starting point for isothiouronium thrombin inhibitors (296) and (297). The boronic ester (296) is prepared by stirring a solution of (291) and thiourea in an inert polar solvent, such as an alcohol or N,N-dimethylformamide, at temperatures ranging from ambient to the reflux temperature of the selected solvent. It is understood that a boronic acid ester like compound (296) is an effective thrombin inhibitor, however, it may be transformed to the corresponding free boronic acid (297) without a loss of biological activity. Compound (297) is derived from the boron ester (296 by transesterification under equilibrium conditions. ##STR76## Thus stirring ester (296) with an excess of an alkyl- or aryl boric acid in a biphasic mixture of neutral or acidic water and an immiscible solvent, such as ethyl ether or toluene, gives (297) after several hours at ambient temperature. The conditions generally preferred use 5 to 10 equivalents of phenylboric acid in ethyl ether/water at neutral pH. Thrombin inhibitors (293) to (299) are obtained by reduction of an azide intermediate prepared from (291) or (292). The azide intermediate is prepared by heating either (291) or (292) with an inorganic azide, such as sodium or potassium azide, in an anhydrous polar aprotic solvent, such as acetone, dimethylformamide or methyl sulfoxide at temperatures ranging from ambient to 130° C. Alternatively, phase transfer conditions may be employed to prepare the azide intermediate from (291) or (292). For example, a tetraalkylammonium azide in a non-polar aprotic solvent, such as tetrahydrofuran or toluene, or a crown ether and inorganic azide in biphasic mixtures of water and an immiscible solvent, such as benzene, toluene or xylene, can be stirred at room temperature or heated up to the reflux point of the selected solvent. The primary amines (293) and (294) are most conveniently obtained from the catalytic hydrogenation of the azide in an inert solvent, such as an alcohol, ethyl acetate or tetrahydrofuran with a transition metal catalyst such as platinum or palladium on carbon under an atmosphere of hydrogen gas. A variety of alternative methods are also useful and can be found in the monograph by Hudlicky (1984, pp. 76). The acid salt of the resulting amines (293) and (294) may be formed by the addition of one equivalent of the desired acid to the hydrogenation mixture. Phenylboric acid mediated hydrolysis of esters (293) and (294) gives the free boronic acid thrombin inhibitors (298) and (299), compounds of formula (I) of the invention.

Compounds containing a primary guanidine or N-alkyl guanidine functionality may be prepared by the alternative process outlined in Scheme 52. As illustrated with primary amine (293), the transformation to (295) is effected with a guanidinylation agent, such as an S-alkyl thiourea, aminoiminomethane sulfonic acid reported by Miller and Bischoff Synthesis 9, 777 (1986), cyanamide reported by Kettner et al. (1990) or their N-alkyl derivatives. This mixture is stirred at room temperature or higher with a base, such as potassium carbonate, triethylamine or N,N-dimethylaminopyridine in an inert solvent like water, alcohol, N,N-dimethylformamide or acetone. The guanidine boronic acid esters (295) can be deesterified to give the corresponding boronic acid (300) by the phenylboric acid procedure described above.

According to Scheme 53, the bromide (292) is converted to the corresponding alkylnitrile (302) upon exposure to the cyanide anion under a variety of conditions. ##STR77## Effective methods include the use of potassium or sodium cyanides in polar aprotic solvents, such as N,N-dimethylformamide, methylsulfoxide, acetone or ethylmethyl ketone, at temperatures ranging from ambient up to the reflux point of the selected solvent. More useful, however, are conditions employing phase transfer agents such as tetrabutylammonium cyanide in a nonpolar aprotic solvent such as tetrahydrofuran or toluene, or a biphasic mixture of a crown ether and an inorganic cyanide in water with an immiscible solvent like benzene, toluene or xylene. These mixtures can be stirred at ambient temperature or heated up to the reflux temperature of the selected solvent. An amidine like (303) is prepared by first treating nitrile (302) with a saturated solution of a mineral acid such as hydrogen chloride in an alcohol solvent at room temperature or lower. The intermediate O-alkylimidate can be exposed to ammonia, or a primary or secondary amine under anhydrous conditions with or without an inert solvent. As illustrated in Scheme 5, compound (303) is produced by treating the O-alkylimidate formed from (302) with neat anhydrous ammonia at reflux. The free boronic acid (304) is obtained by transesterification of (303) with phenylboric acid in a mixture of water and diethyl ether.

EXAMPLE 1 N¹ -(4-Phenylbenzoyl)boroarginine (+)-Pinanediol, Bisulfite

Part A: (+)-Pinanediol 4-bromo-1(R)-(4-phenylbenzo-yl)-aminobutane-1-boronate.

To a solution of (+)-pinanediol 4-bromo-1(R)-aminobutane-1-boronate hydrochloride (5.00 g, 13.6 mmol) in dichloromethane (50 mL) at 0° C. was added 4-phenylbenzoyl chloride (4.97 g, 22.9 mmol) followed by N-methylmorpholine (4 mL, 36 mmol). After 1 hour, the cooling bath was removed and the mixture stirred at room temperature for 2 hours. The mixture was then diluted with ethyl acetate and washed with 0.1M hydrochloric acid, saturated sodium bicarbonate and saturated sodium chloride. The organic phase was dried over anhydrous magnesium sulfate, filtered and the filtrate concentrated in vacuo to afford 3.37 g (48%) of the desired amide, mass spectrum: (M+H)⁺ =510/512; ¹ H NMR (300 MHz, CDCl₃) d7.9 (2H, d, J=8.3), 7.84 (1H, bs), 7.6 (2H, d, J=8.3), 7.44 (5H, m), 4.37 (1H, m), 3.41 (1H, t, J=6.9), 2.0 (10H, m) 1.49 (3H, s), 1.38 (1H, m), 1.29 (3H, s), 0.91 (3H, s).

Part B: (+)-Pinanediol 4-azido-1(R)-(4-phenylbenzo-yl)-aminobutane-1-boronate.

To a solution of (+)-pinanediol 4-bromo-1(R)-(4-phenylbenzoyl)aminobutane-1-boronate (3.37 g, 6.60 mmol) in dimethylformamide (6 mL) was added sodium azide (547 mg, 8.41 mmol). The resulting mixture was heated at 70° C. for 2 hours, cooled to room temperature, and diluted with ethyl acetate. The mixture was then washed with water, saturated sodium chloride and dried over anhydrous magnesium sulfate. Filtration, followed by concentration of the filtrate in vacuo gave 3.04 g (97%) of the desired azide, mass spectrum: (M+H)⁺ =473; ¹ H NMR (300 MHz, CDCl₃) d7.89 (2H, d, J=8.3), 7.75 (1H, bs), 7.3 (7H, m), 4.32 (1H, m), 3.32 (1H, m), 2.0 (10H, m) 1.48 (3H, s), 1.3 (4H, m), 0.9 (3H, s).

Part C: N¹ -(4-Phenylbenzoyl)boroarginine (+)-pinanediol, hydrochloride

To a solution of (+)-pinanediol 4-azido-1(R )--(4-phenylbenzoyl) aminobutane-1-boronate (3.04 g, 6.44 mmol) in methanol (30 mL) was added Pearlman's catalyst (Pd(OH)₂ /C, 200 mg) and 1M hydrochloric acid (6.5 mL, 6.5 mmol). The mixture was placed on a Parr apparatus and hydrogenated at 50 psi for 3 hours. The mixture was filtered using Celite™, washed with methanol and the filtrate concentrated in vacuo. The resulting amorphous solid was dissolved in water and washed with ether. The aqueous phase was then concentrated in vacuo and crystallized from ethyl acetate-hexanes, giving 1.52 g (49%) of the desired amine hydrochloride, mass spectrum: (M+H)⁺ =447; mp: 157°-170° C.; ¹ H NMR (400 MHz, CDCl₃ /DMSO-d₆) d9.88 (1H, bs), 8.18, (2H, d, J=8.3), 8.13 (3H, bs), 7.68 (2H, d, J=8.3), 7.61 (2H, d J=7.0), 7.45 (2H, d, J=7.0), 7.37 (1H, d, J=7.30), 4.20 (1H, d, J=6.3), 2.99 (1H, m), 2.87 (2H, m), 2.31 (1H, m), 2.13 (1H, m), 1.84 (7H, m), 1.56 (1H, d, J=10.0), 1.42 (3H, s), 1.29 (3H, s), 0.89 (3H, s).

Part D: N¹ -(4-Phenylbenzoyl)boroarginine (+)-pinanediol, bisulfite.

To a solution of

N¹ -(4-phenylbenzoyl)boroarginine (+)-pinanediol, hydrochloride (80 mg, 0.17 mmol) in ethanol (2 mL) was added 4-dimethylaminopyridine (40 mg, 0.33 mmol). After 15 minutes, aminoiminomethanesulfonic acid (40 mg, 0.32 mmol) was added and the resulting mixture heated at reflux for 3 hours. After cooling to room temperature, the mixture was filtered and the filtrate concentrated in vacuo. The residue was dissolved in chloroform and washed with 0.1M hydrochloric acid, water and dried over anhydrous magnesium sulfate. Filtration, followed by concentration of the filtrate in vacuo afforded 73 mg (84%) of the desired guanidine, mass spectrum: (M+H)⁺ =489; ¹ H NMR (400 MHz, CDCl₃, 60° C.) d9.48 (1H, bs), 8.10 (2H, d, J=8.1), 8.07 (1H, bs), 7.75 (1H, bs), 7.54 (2H, d, J=8.3), 7.48 (2H, d, J=7.0), 7.35 (3H, m), 7.06 (4H, bs), 4.19 (1H, bd, J=8.3), 3.1 (2H, m), 2.84 (1H, m), 2.29 (1H, m), 2.12 (1H, m), 1.96 (1H, m), 1.75 (6H, m), 1.47 (1H, d, J=10.2), 1.40 (3H, s), 1.24 (3H, s), 0.83 (3H, s).

EXAMPLE 34 (+)-Pinanediol 4-(Formamidino)Thio-1(R)-(4-Phenylbenzoyl)Aminobutane-1-Boronate, Hydrobromide

(+)-Pinanediol 4-(formamidino)thio-1(R)-(4-phenylbenzoyl)aminobutane-1-boronate, hydrobromide.

To a solution of (+)-pinanediol 4-bromo-1(R)-(4-phenyl-benzoyl)aminobutane-1-boronate (200 mg, 0.392 mmol) in methanol (3 mL) was added thiourea (120 mg, 1.58 mmol). The reaction was stirred at room temperature for 3 days. The mixture was concentrated in vacuo, the residue dissolved in water and washed with ether. Concentration of the aqueous portion afforded 80 mg (35%) of the desired isothiourea, mass spectrum: (M+H)⁺ =506; ¹ H NMR (300 MHz, CDCl₃) d8.15 (2H, d, J=8.4), 7.61 (2H, d, J=8.4), 7.52 (2H, m), 7.38 (3H, m), 6.47 (1H, bs), 4.23 (1H, dd, J=6.6, 1.9), 3.24 (1H, m), 3.14, (1H, m), 2.96, (1H, m), 2.32 (1H, m), 2.15 (1H, m), 1.99 (1H, m), 1.78 (6H, m), 1.48 (1H, d, J=10.1), 1.42 (3H, s), 1.27 (3H, s), 0.86 (3H, s). ##STR78##

EXAMPLE 898 R-N¹ -(3-Cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetyl-borolysine, (+)-pinanediol ester, hydrochloride; X=--CH₂ NH₂, R¹³ =--CH₂ Ph, R¹⁴ =--CH₂ CN, Y¹, Y₂ =(+)-pin ##STR79## Part A. Ethyl benzylimidate, hydrochloride.

HCl gas (17.1 g, 469 mmol, 1.1 eq) was slowly bubbled into a solution of phenylacetonitrile (50.00 g, 427 mmol, 1 eq) in ethanol (27.6 mL, 469 mmol, 1.1 eq) at 0° C. The reaction was put into the refrigerator over the weekend. After warming to room temperature, ether (300 mL) was added to the reaction mixture which had solidified and the contents were vigorously stirred at 0° C. to pulverize the mixture. The solid material was filtered while cold under an inert atmosphere and the filter cake rinsed with some more ether. The product was dried under high vacuum to yield 60.0 g (mp 94.0°-95.0° C.) of a white solid. A second crop yielded 20.98 g (96.0°-97.5° C.). ##STR80## Part B. 3-Cyanomethyl-5-phenylmethyl-1,2,4-triazole.

The imidate from part A (14.92 g, 91 mmol, 1 eq) was dissolved in ethanol (250 mL) and cooled to 0° C. under an inert atmosphere. Cyanoacetohydrazide (9.06 g, 91 mmol, 1 eq) dissolved as best possible in warm ethanol was added, and the resultant mixture stirred at room temperature overnight. The mixture was filtered, and the filtrate concentrated to yield a gummy orange solid. Trituration from hexanes yielded 19.72 g of solid product acylamidrazone (MS detects (M+H)⁺ =216). This intermediate was heated neat (oil bath) at 170° C. under an inert atmosphere for 0.5 h to crack out water. The product was cooled to room temperature and dissolved in ethyl acetate. The solvent was dried (MgSO4) and stripped to yield 11.89 g of an orange solid. Flash chromatography over silica gel in solvent systems consisting of 3:1 pentane/ethyl acetate to 100% ethyl acetate to 4:1 chloroform/methanol yielded 6.76 g (38%) of a light pink solid product; m.p.=140.0°-142.5° C. NMR (DMSO-d₆) δ 14.00-13.60 (bs, 1H); 7.40-7.10 (m, 5H); 4.08 (s, 2H); 4.05 (s, 2H). MS: (M+H)⁺ =199. ##STR81## Part C. Ethyl (3-cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetate.

The compound from part B (3.36 g, 17 mmol, 1 eq) was added portionwise to a mixture of DMF and 50% NaH (0.81 g, 17 mmol, 1 eq) at 25° C. After H₂ evolution had ceased, the mixture was heated a little with a heat gun to ensure complete deprotonation. The mixture was cooled to 0° C. and ethyl bromoacetate (1.88 mL, 17 mmol, 1 eq ) was added. The reaction was allowed to warm to room temperature and was stirred overnight. Ethyl acetate was added and the mixture washed with water (5×) to remove the DMF. The organic layer was dried (MgSO₄) and stripped to yield 6.10 g of a reddish oil. Flash chromatography in 3:1 hexanes/ethyl acetate to 1:1 hexanes/ethyl acetate yielded 2.93 g of an amber oil which consisted of a 4:1 mixture of regioisomers as determined by NMR with the major isomer being depicted above. NMR (major isomer) (CDCl₃) δ 7.40-7.20 (m, 5H); 4.68 (s, 2H); 4.25-4.05 (m, 4H); 3.84 (s, 2H); 1.23 (t, 3H, J=7 Hz). ##STR82## Part D. (3-Cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetate acid.

The product of part C (1.00g, 3.52 mmol, 1 eq), 1.000N NaOH (7.03 mL, 7.03 mmol, 2 eq) and methanol (10 mL) were mixed and stirred at room temperature. After 24 h, the methanol was stripped and the aqueous mixture washed with ether (2x). The aqueous layer was then acidified with conc. HCl and extracted with ethyl acetate (3×). The organic layers were combined, dried (MgSO₄) and stripped to yield 0.66 g of an off-white glass. MS (M+H)⁺ =257. ##STR83## Part E. (+)-Pinanediol 5bromo-1(R)-((3-Cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetamido)pentane-1-boronate.

N-methylmorpholine (0.42 mL, 3.86 mmol, 1.5 eq) was added to a solution of the product in part D (0.66 g, 2.58 mmol, 1 eq) in THF at 25° C. The mixture was cooled to -20° C. and isobutylchloroformate (0.50 mL, 3.86 mmol, 1.5 eq) in THF was added dropwise. In a seperate flask, pinanediol 5-bromo-1-R-aminopentane-1-boronate hydrochloride (0.98 g, 2.58 mmol, 1 eq) was dissolved in CHCl₁₃ and cooled to -78° C. Triethylamine (0.36 mL, 2.58 mmol, 1 eq) was then added and the mixture syringed immediately into the reaction flask with the mixed anhydride. The reaction was allowed then to warm to room temperature overnight. The next day, the precipitate was filtered off and the solids were rinsed with THF. The filtrate was stripped to yield 410 mg of a white oil. Flash chromatography over silica gel in solvent systems consisting of 3:1 pentane/ethyl acetate to 100% ethyl acetate to 4:1 chloroform/methanol yielded 300 mg of a clear, colorless viscous oil and only one regioisomer by NMR. MS (M+H)⁺ =633 and 635. NMR (CDCl₃) δ 7.40-7.10 (m, 5H); 6.13 (d, 1H, J=6 Hz); 4.62 (s, 2H); 4.40-4.20 (m, 1H); 4.17 (s, 2H); 3.86 (s, 1H); 3.50-3.20 (m, 3H); 2.40-2.10 (m, 2H); 2.10-1.75 (m, 4H); 1.75-1.10 (m, 13 H); 0.83 (s, 3H). ##STR84## Part F. (+)-Pinanediol 5bromo-1(R)-((3-Cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetamido)pentane-1-boronate.

The product from Part E (300 mg, 0.52 mmol, 1 eq), sodium azide (1.03 mmol, 2 eq), and DMSO (5 mL) were mixed and stirred at room temperature under an inert atmosphere for 24 h. Ethyl acetate was added and the mixture rinsed with water (5×). The ethyl acetate layer was dried (MgSO₄) and stripped to yield 256 mg of a light amber oil. IR (neat)₂₀₉₆ cm-1. NMR (CDCl3) δ 7.40-7.10 (m, 5H); 6.15 (d, 1H, J=6 Hz); 4.62 (s, 2H); 4.40-4.20 (d of d, 1H, J=7, 2 Hz); 4.20-4.10 (m, 2H); 3.85 (s, 2H); 3.40-3.10 (m, 3H); 2.50-1.40 (m, 9H); 1.40-1.00 (m, 9 H); 0.84 (s, 3H). ##STR85## Part G. (+)-Pinanediol 5bromo-1(R)-((3-Cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetamido)pentane-1-boronate, hydrochloride salt.

The product from Part F (250 mg, 0.46mmol, 1 eq) and triphenylphosphine (157 mg, 0.6 mmol, 1.3 eq) and THF (5 mL) were mixed and stirred at room temperature. After 1 h, water (11 μM, 0.6 mmol, 1.3 eq) was added and the mixture stirred overnight. After 24 h, the reaction was not finished, and thus 1.3 eq more equivalents of water were added and the reaction stirred for another 24 h. The reaction was now complete and 1 equivalent of 1.000N HCl was added. The reaction was then stripped and water was added and the reaction again stripped. Ethyl ether was added and the mixture stripped once more. The residue was dried under high vacuum to yield 138 mg of a white glass. MS detects (M+H)⁺ =519 and 385 (minus pinanediol). Mass calculated for C₂₈ H₄₀ BN₆ O₃ : 519.3255. Found: 519.3274. NMR shows a 1:1 mixture of pinanediol ester and free boronic acid. ##STR86##

EXAMPLE 908 R-N¹ -(3-(1H-tetrazol-5-yl)methyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetyl-borolysine, (+)-pinanediol ester, hydrochloride; X=--CH₂ NH₂, R¹³ =--CH₂ Ph, R¹⁴ =--CH₂ --(CN⁴ H), Y¹, Y² =(+)-pin ##STR87## Part A. Ethyl (3)-N-triphenylmethyl)-1H-tetrazol-5-methyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetate

The product from Example 360, part C (1.83 g, 6.44 mmol, 1 eq), tributyltin chloride (1.75 mL, 6.44 mmol, 1 eq), sodium azide (0.42 g, 6.44 mmol, 1 eq), and xylenes (15 mL) were mixed and refluxed for 24 h under an inert atmosphere. The mixture was cooled to room temperature and pyridine was then added (0.57 mL, 7.08 mmol, 1.1 eq) followed after 0.5 h by trityl chloride (1.97 g, 7.08 mmol, 1.1 eq). The following day, the reaction was worked up by adding ethyl ether and rinsing the mixture with water (3×). The ether layer was dried (MgSO4), and stripped to yield 5.66 g of an amber oil. Flash chromatography in 3:1 pentane/ethyl acetate to 100% ethyl acetate over silica gel yielded 1.33 g of an amber oil which eventually crystallized. MS detects (M+H)⁺ =570 and 328 (M+H--CPh₃)⁺. ##STR88## Part B. (3)-N-Triphenylmethyl)-1H-tetrazol-5-yl)methyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetic acid.

The product from part A (200 mg, 0.35 mmol, 1 eq), 1,000N NaOH (0.39 mL, 0.39 mmol, 1.1 eq) and THF (5 mL) were mixed and stirred at room temperature under an inert atmosphere for 24 h. The reaction was not finished and thus 0.5 eq more of 1,000N NaOH were added and stirred overnight. Water was then added and the pH adjusted to 5 with 1N HCl . The mixture was stripped to dryness. THe residue was stirred in ethyl acetate. Some solids were filtered and the filtrate was stripped to yield 190 mg of a white glass. NMR (CDCl₃) δ 7.40-7.15 (m, 12 H); 7.15-7.00 (m, 8 H); 4.55 (s, 2); 4.40 (s, 2H); 4.10 (s, 2H). ##STR89## Part C. (+)-Pinanediol 5-azido-1(R)-((3-N-triphenylmethyl)-1H-tetrazol-5-ylmethyl-)5-phenylmethyl1,2,4-triazol-1-yl)acetamido)pentane-1-boronate.

The compound in part B was converted to the corresponding azidoboronic acid pinanediol ester by the methods disclosed in example 360, parts E and F. IR (neat) 2095 cm⁻¹. NMR (CDCl₃) δ 7.45-7.20 (m, 12H); 7.17 (d, 2H, J=7 Hz); 7.12 (d, 6H, J=7 Hz); 6.34 (d, 1H, J=6 Hz); 4.60 (s, 2H); 4.42 (s, 2H); 4.27 (d, 1H, J=7 Hz); 3.13 (t, 2H, J=2 Hz); 3.06 (q, 1H, J=7 Hz); 2.40-2.10 (m, 2H); 2.01 (t, 1H, J=6 Hz); 1.95-1.70 (m, 2H); 1.60-1.40 (m, 4H); 1.37 (s, 3H); 1.35-1.20 (m, 5H); 1.16 (d, 1H, J=11 Hz); 0.82 (s, 3H). MS detects (M+H)⁺ =830 and (M+H--CPh₃)⁺ =588. ##STR90## Part D. R-N¹ -(3-(1H-tetrazol-5-yl)methyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetyl-borolysine, (+)-pinanediol ester, hydrochloride.

The product from part C (135 mg, 0.16 mmol, 1 eq), 10% Pd on carbon (25 mg), chloroform (39 μL, 0.49 mmol, 3 eq) and methanol (5 mL) were mixed and stirred under hydrogen under balloon pressure for 24 h at room temperature. The mixture was filtered through a Celite® cake rinsing the cake well with methanol afterwards. The filtrate was stripped to yield an off-white glass. This glass was triturated with ethyl ether to yield after drying 50 mg of an off-white solid. Mass calcd. for C₂₈ H₄₁ BN⁹ O₃ : 562.3425. Found: 562.3413. NMR (DMSO-d₆) δ 8.75-8.50 (m, 1H); 7.40-7.10 (m, 5H); 4.87 (bs, 2H); 4.30-4.00 (m, 5H); 2.96-2.60 (m, 3H); 2.40-2.00 (m, 2H); 1.91 (t, 1H, J=6 Hz); 1.90-1.75 (m, 1H); 1.75-1.10 (m, 14 H); 0.80 (s, 3H). ##STR91##

EXAMPLE 3458 R-N¹ -((2-phenyl-4-methylpyrimidin-5-yl)carbonyl)borolysine, (+)-pinanediol ester, hydrochloride; X=--CH₂ NH₂, R¹³ =--Ph, R¹⁴ =--CH₃, R¹⁵ =H, Y¹, Y² =(+)-pin ##STR92## Part A. 2-Phenyl-4-methylpyrimidin-5-carboxylic acid.

The above compound was synthesized by the procedure of P. Schenone, L. Sansebastiano, L. Mosti J. Heterocyclic Chem. 1990, 27, 302 which is generally applicable to a wide variety of pyrimidine-5-carboxylic acids.

Part B. R-N¹ -((2-phenyl-4-methylpyrimidine-5-yl)carbonyl)borolysine, (+)-pinanediol ester, hydrochloride.

The product was obtained using the procedures described in example 360, parts E and F and example 361, part D followed by prepatory TLC in 4:1 chloroform/methanol. (M+H)⁺ =477. NMR (DMSO-d₆) δ 8.86 (s, 1H); 8.50-8.30 (m, 2H); 7.70-7.40 (m, 3H); 4.25 (d, 1H, J=7 Hz); 2.90-2.70 (m, 3H); 2.64 (s, 3H); 2.40-1.00 (m, 15H); 0.84 (s, 3H). ##STR93##

EXAMPLE 3538 R-N¹ -((2-phenyl-4-methylpyrimidin-5-yl)carbonyl)boroarginine, (+)-pinanediol ester, hydrochloride; X=--NH (C═NH) NH₂, R¹³ =--Ph, R¹⁴ =--CH₃, R¹⁵ =H, Y¹, Y² =(+)-pin ##STR94## Part A. R-N¹ -((2-phenyl-4-methylpyrimidin-5-yl)carbonyl)boroarginine, (+)-pinanediol ester, hydrochloride.

The above intermediate was synthesized by the procedures described for example 361 using the appropriate starting materials.

Part B. R-N¹ -((2-phenyl-4-methylpyrimidin-5-yl)carbonyl)boroarginine, (+)-pinanediol ester, hydrochloride.

The product from part A (500 mg, 1 mmol, 1 eq), formamidinesulfonic acid (224 mg, 1.8 mmol, 2 eq), 4-(N,N-dimethylamino)pyridine (220 mg, 1.8 mmol, 2 eq, and ethanol (20 mL) were mixed and refluxed under an inert atmosphere for 5 hours. Some solid material was filtered and the filtrate was stripped to yield a yellow glass. The glass was taken up in chloroform/0.1N HCl. Solids precipitated. These were filtered and dried to yield 144 mg of product as a white powder: mp 132° C. (dec.). (M+H)⁺⁼ 505.

Mass calcd. for C₂₇ H₃₈ BN₆ O₃ : 505.3086. Found: 505.3098. NMR (DMSO-d₆) δ 8.89 (s, 1H); 8.60-8.40 (m, 2H); 8.05-7.80 (m, 1H); 7.65-7.40 (m, 3H); 7.40-6.80 (m, 3H); 4.19 (d, 1H, J=7 HZ); 3.60-3.20 (m, 3H); 2.85-2.40 (m, 4H); 2.40-1.95 (m, 1H); 1.95-1.00 (m, 16 H); 0.80 (t, 3H). ##STR95##

EXAMPLE 5926 N¹ - (4R)-2-(2-Phenyl)ethyl-Thiazoline-4-Carboxy!-R-borothioarginine-(+)-pinanediol ester

Part A. (4R )-2-(2-phenyl)-thiazoline-4-carboxylic acid ethyl ester.

Cysteine ethyl ester hydrochloride (950 mg, 5.10 mmol) was added to a solution of ethyl (2-phenyl)ethylimidate (900 mg, 5.10 mmol) prepared by the method of North, M.; Pattenden, G. Tetrahedron 1990, 46, 8267! in EtOH (20 mL) at room temperature. The reaction mixture was stirred for 16 h and concentrated under reduced pressure. The residue was partitioned between H₂ O (ca. 50 mL) and EtOAc (ca. 100 mL) and the layers were separated; the aqueous phase was extracted with EtOAc (1×20 mL). The combined organic layers were washed with saturated aqueous NaCl₁ (1×50 mL), dried (Na₂ SO₄), and concentrated under reduced pressure to give an oil which was purified by flash chromatography, elution with 3:1 hexanes--EtOAc, to afford 885 mg (66%) of the title compound as a colorless oil. ¹ H NMR (300 MHz, CDCl₃) δ 7.23 (comp, 5H), 5.05 (dd, 1H, J=9.5, 9.1 Hz), 4.27 (dq, 2H, J=7.0, 1.8 Hz), 3.55 (m, 2H), 2.97 (m, 2H), 2.86 (m, 2H), 1.32 (t, 3H, J=7.0 Hz); LRMS 264 (M+1, base).

Part B. (4R)-2-(2-phenyl)ethyl-thiazoline-4carboxylic acid.

A solution of lithium hydroxide monohydrate (96 mg, 2.28 mmol) in H₂ O (2 mL) was added to a solution of (4R)-2-(2-phenyl)ethyl-thiazoline-4-carboxylic acid ethyl ester (400 mg, 1.52 mmol) in THF (8 mL) and MeOH (5 mL). The reaction mixture was stirred at room temperature for 1 h at which time 2M aqueous HCl was added until pH=2 and the aqueous phase was extracted with EtOAc (2-30 mL). The combined organic layers were washed with saturated aqueous NaCl (1-20 mL), dried (MgSO₄), and concentrated under reduced pressure to give 340 mg (95%) of the title compound as an oil. ¹ H NMR (300 MHz, CDCl₃) δ 7.22 (comp, 5H), 6.86 (br s, 1H), 5.14 (dd, 1H, J=9.5, 9.1 Hz), 3.64 (m, 2H), 2.96 (comp, 4H); LRMS 236 (M+1, base).

Part C. (1R)-4-Bromo-1- (4R)-2-(2-Phenyl)ethyl-thiazoline-4carbox!amido-1-boronic acid-(+)-pinanediol ester.

A solution of (4R)-2-(2-phenyl)ethyl-thiazoline-4-carboxylic acid (335 mg, 1.43 mmol) and 4-methylmorpholine (0.47 mL, 4.28 mmol) in 10 mL of anhydrous THF at -20° C. was treated with i--butyl chloroformate (0.20 mL, 1.57 mmol) and stirred for 2 min after which a solution of (1R)-4-bromoaminobutane-1-boronic acid (+)-pinanediol ester (522 mg, 1.43 mmol) in 4 mL of anhydrous DMF was added. The reaction mixture was stirred at -20° C. for 15 min, warmed to room temperature over 18 h then poured into EtOAc (ca. 100 mL) and washed with H₂ O (3-25 mL), and saturated aqueous NaCl (1-25 mL), dried (Na₂ SO₄) and concentrated under reduced pressure. The residue was purified by flash chromatography, elution with 3:2 hexanes--EtOAc, to give 306 mg (39%) of the title compound as an oil. LRMS 549, 547 (M+1, base).

Part D. N¹ - (4R -2-2-Phenyl)ethyl-Thiazoline-4-Carboxy!-R-borothioarginine-(+)-pinanediol ester.

A mixture of (1R)-4-bromo-1- (4R)-2-(2 -phenyl)ethyl-thiazoline-4-carbox!amido-1-boronic acid (+)-pinanediol ester (295 mg, 0.54 mmol) and thiourea (82 mg, 1.08 mmol) in 10 mL of EtOH was heated at reflux for 14 h then cooled to room temperature and concentrated under reduced pressure. The residue was purified by size exclusion chromatography on Sephadex LH-20, elution with MeOH, to give a glass which was dissolved in 3 mL of THF and treated with Et₂ O (ca. 10 mL) to give a solid that was washed with Et₂ O (ca. 5 mL) and dried to afford 230 mg (68%) of the title compound. LRMS 543 (M+1, base); HRMS Calcd for C₂₇ H₄₀ BN₄ O₃ S₂ : 543.2635. Found: 543.2643.

The compounds in the following tables were or can be synthesized by the methods discussed previously or by methods familiar to one skilled in the art.

The compounds listed in Tables 1-61 may be prepared using the above examples. It is understood that R¹⁴⁻¹⁶ and R^(A-C) in the tables correspond to independent R13 groups as described within the scope of this application.

                                      TABLE 1                                      __________________________________________________________________________      ##STR96##                                                                     Ex X       R.sup.A  R.sup.B  R.sup.C      Y.sup.1, Y.sup.2                                                                    Phys Data                       __________________________________________________________________________     1  NHC(NH)NH.sub.2                                                                        H        H        Ph           (+)-pin                                                                             A                               2  NHC(NH)NH.sub.2                                                                        H        Ph       H            (+)-pin                                                                             BZ                              3  NHC(NH)NH.sub.2                                                                        H        OPh      Ph           (+)-pin                                                                             B                               4  NHC(NH)NH.sub.2                                                                        H        H        4-pyridyl    (+)-pin                                                                             C                               5  NHC(NH)NH.sub.2                                                                        COPh     H        H            (+)-pin                              6  NHC(NH)NH.sub.2                                                                        H        COPh     H            (+)-pin                              7  NHC(NH)NH.sub.2                                                                        H        H        COPh         (+)-pin                              8  NHC(NH)NH.sub.2                                                                        H        NHCbz    H            (+)-pin                              9  NHC(NH)NH.sub.2                                                                        H        NMeCbz   H            (+)-pin                              10 NHC(NH)NH.sub.2                                                                        H        H        Et           (+)-pin                              11 NHC(NH)NH.sub.2                                                                        H        H        n-Pr         (+)-pin                              12 NHC(NH)NH.sub.2                                                                        H        H        i-Pr         (+)-pin                              13 NHC(NH)NH.sub.2                                                                        H        H        n-Bu         (+)-pin                              14 NHC(NH)NH.sub.2                                                                        H        H        t-Bu         (+)-pin                              15 NHC(NH)NH.sub.2                                                                        H        H        n-hexyl      (+)-pin                              16 NHC(NH)NH.sub.2                                                                        H        H        cyclohexyl   (+)-pin                              17 NHC(NH)NH.sub.2                                                                        NHCO(CH.sub.2).sub.2 Ph                                                                 H        H            (+)-pin                              18 NHC(NH)NH.sub.2                                                                        H        H        O-n-Bu       (+)-Pin                              19 NHC(NH)NH.sub.2                                                                        H        H        NHCOcyclopropyl                                                                             (+)-pin                              20 NHC(NH)NH.sub.2                                                                        H        H        NHCO-cyclohexyl                                                                             (+)-pin                              21 NHC(NH)NH.sub.2                                                                        H        H        NHCO(4-C.sub.6 H.sub.4 OMe)                                                                 (+)-pin                              22 NHC(NH)NH.sub.2                                                                        H        H        4-C.sub.6 H.sub.4 OMe                                                                       (+)-pin                              23 NHC(NH)NH.sub.2                                                                        CO.sub.2 CH.sub.2 (2-C.sub.6 H.sub.4 Ph)                                                H        H            (+)-pin                              24 NHC(NH)NH.sub.2                                                                        H        H        1-naphthyl   (+)-pin                              25 NHC(NH)NH.sub.2                                                                        H        H        4-C.sub.6 H.sub.4 CO.sub.2 H                                                                (+)-pin                              26 NHC(NH)NH.sub.2                                                                        COPh     H        Me           (+)-pin                              27 NHC(NH)NH.sub.2                                                                        H        NHCbz    n-Bu         (+)-pin                              28 NHC(NH)NH.sub.2                                                                        H        NMeCbz   n-Bu         (+)-pin                              29 NHC(NH)NH.sub.2                                                                        Me       H        Ph           (+)-pin                                                                             CB                              30 NHC(NH)NH.sub.2                                                                        Me       H        4-C.sub.6 H.sub.4 CO.sub.2 H                                                                (+)-pin                              31 NHC(NH)NH.sub.2                                                                        H        H        4-C.sub.6 H.sub.4 CO.sub.2 Me                                                               (+)-pin                              32 NHC(NH)NH.sub.2                                                                        Me       H        4-C.sub.6 H.sub.4 CO.sub.2 Me                                                               (+)-pin                              33 NHC(NH)NH.sub.2                                                                        H        OMe      Ph           (+)-pin                              34 SC(NH)NH.sub.2                                                                         H        H        Ph           (+)-pin                                                                             D                               35 SC(NH)NH.sub.2                                                                         H        Ph       H            (+)-pin                                                                             E                               36 SC(NH)NH.sub.2                                                                         H        OPh      H            (+)-pin                                                                             F                               37 SC(NH)NH.sub.2                                                                         COPh     H        H            (+)-pin                                                                             G                               38 SC(NH)NH.sub.2                                                                         H        COPh     H            (+)-pin                                                                             H                               39 SC(NH)NH.sub.2                                                                         H        H        COPh         (+)-pin                                                                             I                               40 SC(NH)NH.sub.2                                                                         H        NHCbz    H            (+)-pin                                                                             J                               41 SC(NH)NH.sub.2                                                                         H        NMeCbz   H            (+)-pin                                                                             K                               42 SC(NH)NH.sub.2                                                                         H        H        Et           (+)-pin                                                                             L                               43 SC(NH)NH.sub.2                                                                         H        H        n-Pr         (+)-pin                                                                             M                               44 SC(NH)NH.sub.2                                                                         H        H        i-Pr         (+)-pin                                                                             N                               45 SC(NH)NH.sub.2                                                                         H        H        n-Bu         (+)-pin                                                                             O                               46 SC(NH)NH.sub.2                                                                         H        H        t-Bu         (+)-pin                                                                             P                               47 SC(NH)NH.sub.2                                                                         H        H        n-hexyl      (+)-pin                                                                             Q                               48 SC(NH)NH.sub.2                                                                         H        H        cyclohexyl   (+)-pin                                                                             R                               49 SC(NH)NH.sub.2                                                                         NHCOCH.sub.2 CH.sub.2 Ph                                                                H        H            (+)-pin                                                                             S                               50 SC(NH)NH.sub.2                                                                         H        H        O-n-Bu       (+)-pin                                                                             P                               51 SC(NH)NH.sub.2                                                                         H        H        NHCOcyclopropyl                                                                             (+)-pin                                                                             U                               52 SC(NH)NH.sub.2                                                                         H        H        NHCOcyclohexyl                                                                              (+)-pin                                                                             V                               53 SC(NH)NH.sub.2                                                                         H        H        NHCO(4-C.sub.6 H.sub.4 OMe)                                                                 (+)-pin                                                                             W                               54 SC(NH)NH.sub.2                                                                         H        H        4-C.sub.6 H.sub.4 OMe                                                                       (+)-pin                                                                             X                               55 SC(NH)NH.sub.2                                                                         CO.sub.2 CH.sub.2 (2-C.sub.6 H.sub.4 Ph)                                                H        H            (+)-pin                                                                             Y                               56 SC(NH)NH.sub.2                                                                         H        H        1-naphthyl   (+)-pin                              57 SC(NH)NH.sub.2                                                                         H        H        4-C.sub.6 H.sub.4 CO.sub.2 H                                                                (+)-pin                              58 SC(NH)NH.sub.2                                                                         H        NHCbz    n-Bu         (+)-pin                                                                             Z                               59 SC(NH)NH.sub.2                                                                         H        NMeCbz   n-Bu         (+)-pin                                                                             AA                              60 SC(NH)NH.sub.2                                                                         COPh     H        Me           (+)-pin                                                                             BB                              61 SC(NH)NH.sub.2                                                                         H        H        4-pyridyl    (+)-pin                              62 SC(NH)NH.sub.2                                                                         Me       H        4-C.sub.6 H.sub.4 CO.sub.2 H                                                                (+)-pin                              63 SC(NH)NH.sub.2                                                                         H        H        4-C.sub.6 H.sub.4 CO.sub.2 Me                                                               (+)-pin                              64 SC(NH)NH.sub.2                                                                         Me       H        4-C.sub.6 H.sub.4 CO.sub.2 Me                                                               (+)-pin                              65 SC(NH)NH.sub.2                                                                         Me       H        Ph           (+)-pin                              66 SC(NH)NH.sub.2                                                                         H        OMe      Ph           (+)-pin                              67 CH.sub.2 NH.sub.2                                                                      H        H        Ph           (+)-pin                              68 CH.sub.2 NH.sub.2                                                                      H        Ph       H            (+)-pin                                                                             YY                              69 CH.sub.2 NH.sub.2                                                                      H        OPh      H            (+)-pin                              70 CH.sub.2 NH.sub.2                                                                      COPh     H        H            (+)-pin                              71 CH.sub.2 NH.sub.2                                                                      H        COPh     H            (+)-pin                              72 CH.sub.2 NH.sub.2                                                                      H        H        COPh         (+)-pin                              73 CH.sub.2 NH.sub.2                                                                      H        NHCbz    H            (+)-pin                              74 CH.sub.2 NH.sub.2                                                                      H        NMeCbz   H            (+)-pin                              75 CH.sub.2 NH.sub.2                                                                      H        H        Et           (+)-pin                              76 CH.sub.2 NH.sub.2                                                                      H        H        n-Pr         (+)-pin                              77 CH.sub.2 NH.sub.2                                                                      H        H        i-Pr         (+)-pin                              78 CH.sub.2 NH.sub.2                                                                      H        H        n-Bu         (+)-pin                              79 CH.sub.2 NH.sub.2                                                                      H        H        t-Bu         (+)-pin                              80 CH.sub.2 NH.sub.2                                                                      H        H        n-hexyl      (+)-pin                              81 CH.sub.2 NH.sub.2                                                                      H        H        cyclohexyl   (+)-pin                              82 CH.sub.2 NH.sub.2                                                                      NHCOCH.sub.2 CH.sub.2 Ph                                                                H        H            (+)-pin                              83 CH.sub.2 NH.sub.2                                                                      H        H        O-n-Bu       (+)-pin                              84 CH.sub.2 NH.sub.2                                                                      H        H        NHCOcyclopropyl                                                                             (+)-pin                              85 CH.sub.2 NH.sub.2                                                                      H        H        NHCOcyclohexyl                                                                              (+)-pin                              86 CH.sub.2 NH.sub.2                                                                      H        H        NHCO(4-C.sub.6 H.sub.4 OMe)                                                                 (+)-pin                              87 CH.sub.2 NH.sub.2                                                                      H        H        4-C.sub.6 H.sub.4 OMe                                                                       (+)-pin                              88 CH.sub.2 NH.sub.2                                                                      CO.sub.2 CH.sub.2 (2-C.sub.6 H.sub.4 Ph)                                                H        H            (+)-pin                              89 CH.sub.2 NH.sub.2                                                                      H        H        1-naphthyl   (+)-pin                              90 CH.sub.2 NH.sub.2                                                                      H        H        4-C.sub.6 H.sub.4 CO.sub.2 H                                                                (+)-pin                              91 CH.sub.2 NH.sub.2                                                                      H        NHCbz    n-Bu         (+)-pin                              92 CH.sub.2 NH.sub.2                                                                      H        NMeCbz   n-Bu         (+)-pin                              93 CH.sub.2 NH.sub.2                                                                      COPh     H        Me           (+)-pin                              94 CH.sub.2 NH.sub.2                                                                      H        H        4-pyridyl    (+)-pin                              95 CH.sub.2 NH.sub.2                                                                      Me       H        4-C.sub.6 H.sub.4 CO.sub.2 H                                                                (+)-pin                              96 CH.sub.2 NH.sub.2                                                                      H        H        4-C.sub.6 H.sub.4 CO.sub.2 Me                                                               (+)-pin                              97 CH.sub.2 NH.sub.2                                                                      Me       H        4-C.sub.6 H.sub.4 CO.sub.2 Me                                                               (+)-pin                              98 CH.sub.2 NH.sub.2                                                                      Me       H        Ph           (+)-pin                              99 CH.sub.2 NH.sub.2                                                                      H        OMe      Ph           (+)-pin                              100                                                                               CH.sub.2 NH.sub.2                                                                      H        OMe      Ph           OH, OH                               101                                                                               NHC(NH)NH.sub.2                                                                        H        H        Ph           OH, OH                               102                                                                               NHC(NH)NH.sub.2                                                                        H        Ph       H            OH, OH                               103                                                                               NHC(NH)NH.sub.2                                                                        H        OPh      Ph           OH, OH                               104                                                                               NHC(NH)NH.sub.2                                                                        H        H        4-pyridyl    OH, OH                               105                                                                               NHC(NH)NH.sub.2                                                                        COPh     H        H            OH, OH                               106                                                                               NHC(NH)NH.sub.2                                                                        H        COPh     H            OH, OH                               107                                                                               NHC(NH)NH.sub.2                                                                        H        H        COPh         OH, OH                               108                                                                               NHC(NH)NH.sub.2                                                                        H        NHCbz    H            OH, OH                               109                                                                               NHC(NH)NH.sub.2                                                                        H        NMeCbz   H            OH, OH                               110                                                                               NHC(NH)NH.sub.2                                                                        H        H        Et           OH, OH                               111                                                                               NHC(NH)NH.sub.2                                                                        H        H        n-Pr         OH, OH                               112                                                                               NHC(NH)NH.sub.2                                                                        H        H        i-Pr         OH, OH                               113                                                                               NHC(NH)NH.sub.2                                                                        H        H        n-Bu         OH, OH                               114                                                                               NHC(NH)NH.sub.2                                                                        H        H        t-Bu         OH, OH                               115                                                                               NHC(NH)NH.sub.2                                                                        H        H        n-hexyl      OH, OH                               116                                                                               NHC(NH)NH.sub.2                                                                        H        H        cyclohexyl   OH, OH                               117                                                                               NHC(NH)NH.sub.2                                                                        NHCO(CH.sub.2).sub.2 Ph                                                                 H        H            OH, OH                               118                                                                               NHC(NH)NH.sub.2                                                                        H        H        O-n-Bu       OH, OH                               119                                                                               NHC(NH)NH.sub.2                                                                        H        H        NHCOcyclopropyl                                                                             OH, OH                               120                                                                               NHC(NH)NH.sub.2                                                                        H        H        NHCO-cyclohexyl                                                                             OH, OH                               121                                                                               NHC(NH)NH.sub.2                                                                        H        H        NHCO(4-C.sub.6 H.sub.4 OMe)                                                                 OH, OH                               122                                                                               NHC(NH)NH.sub.2                                                                        H        H        4-C.sub.6 H.sub.4 OMe                                                                       OH, OH                               123                                                                               NHC(NH)NH.sub.2                                                                        CO.sub.2 CH.sub.2 (2-C.sub.6 H.sub.4 Ph)                                                H        H            OH, OH                               124                                                                               NHC(NH)NH.sub.2                                                                        H        H        1-naphthyl   OH, OH                               125                                                                               NHC(NH)NH.sub.2                                                                        H        H        4-C.sub.6 H.sub.4 CO.sub.2 H                                                                OH, OH                               126                                                                               NHC(NH)NH.sub.2                                                                        COPh     H        Me           OH, OH                               127                                                                               NHC(NH)NH.sub.2                                                                        H        NHCbz    n-Bu         OH, OH                               128                                                                               NHC(NH)NH.sub.2                                                                        H        NMeCbz   n-Bu         OH, OH                               129                                                                               NHC(NH)NH.sub.2                                                                        Me       H        Ph           OH, OH                                                                              CD                              130                                                                               NHC(NH)NH.sub.2                                                                        Me       H        4-C.sub.6 H.sub.4 CO.sub.2 H                                                                OH, OH                               131                                                                               NHC(NH)NH.sub.2                                                                        H        H        4-C.sub.6 H.sub.4 CO.sub.2 Me                                                               OH, OH                               132                                                                               NHC(NH)NH.sub.2                                                                        Me       H        4-C.sub.6 H.sub.4 CO.sub.2 Me                                                               OH, OH                               133                                                                               NHC(NH)NH.sub.2                                                                        H        OMe      Ph           OH, OH                               134                                                                               SC(NH)NH.sub.2                                                                         H        H        Ph           OH, OH                               135                                                                               SC(NH)NH.sub.2                                                                         H        Ph       H            OH, OH                               136                                                                               SC(NH)NH.sub.2                                                                         H        OPh      H            OH, OH                               137                                                                               SC(NH)NH.sub.2                                                                         COPh     H        H            OH, OH                               138                                                                               SC(NH)NH.sub.2                                                                         H        COPh     H            OH, OH                               139                                                                               SC(NH)NH.sub.2                                                                         H        H        COPh         OH, OH                               140                                                                               SC(NH)NH.sub.2                                                                         H        NHCbz    H            OH, OH                               141                                                                               SC(NH)NH.sub.2                                                                         H        NMeCbz   H            OH, OH                               142                                                                               SC(NH)NH.sub.2                                                                         H        H        Et           OH, OH                               143                                                                               SC(NH)NH.sub.2                                                                         H        H        n-Pr         OH, OH                               144                                                                               SC(NH)NH.sub.2                                                                         H        H        i-Pr         OH, OH                               145                                                                               SC(NH)NH.sub.2                                                                         H        H        n-Bu         OH, OH                               146                                                                               SC(NH)NH.sub.2                                                                         H        H        t-Bu         OH, OH                               147                                                                               SC(NH)NH.sub.2                                                                         H        H        n-hexyl      OH, OH                               148                                                                               SC(NH)NH.sub.2                                                                         H        H        cyclohexyl   OH, OH                               149                                                                               SC(NH)NH.sub.2                                                                         NHCOCH.sub.2 CH.sub.2 Ph                                                                H        H            OH, OH                               150                                                                               SC(NH)NH.sub.2                                                                         H        H        O-n-Bu       OH, OH                               151                                                                               SC(NH)NH.sub.2                                                                         H        H        NHCOcyclopropyl                                                                             OH, OH                               152                                                                               SC(NH)NH.sub.2                                                                         H        H        NHCOcyclohexyl                                                                              OH, OH                               153                                                                               SC(NH)NH.sub.2                                                                         H        H        NHCO(4-C.sub.6 H.sub.4 OMe)                                                                 OH, OH                               154                                                                               SC(NH)NH.sub.2                                                                         H        H        4-C.sub.6 H.sub.4 OMe                                                                       OH, OH                               155                                                                               SC(NH)NH.sub.2                                                                         CO.sub.2 CH.sub.2 (2-C.sub.6 H.sub.4 Ph)                                                H        H            OH, OH                               156                                                                               SC(NH)NH.sub.2                                                                         H        H        1-naphthyl   OH, OH                               157                                                                               SC(NH)NH.sub.2                                                                         H        H        4-C.sub.6 H.sub.4 CO.sub.2 H                                                                OH, OH                               158                                                                               SC(NH)NH.sub.2                                                                         H        NHCbz    n-Bu         OH, OH                               159                                                                               SC(NH)NH.sub.2                                                                         H        NMeCbz   n-Bu         OH, OH                               160                                                                               SC(NH)NH.sub.2                                                                         COPh     H        Me           OH, OH                               161                                                                               SC(NH)NH.sub.2                                                                         H        H        4-pyridyl    OH, OH                               162                                                                               SC(NH)NH.sub.2                                                                         Me       H        4-C.sub.6 H.sub.4 CO.sub.2 H                                                                OH, OH                               163                                                                               SC(NH)NH.sub.2                                                                         H        H        4-C.sub.6 H.sub.4 CO.sub.2 Me                                                               OH, OH                               164                                                                               SC(NH)NH.sub.2                                                                         Me       H        4-C.sub.6 H.sub.4 CO.sub.2 Me                                                               OH, OH                               165                                                                               SC(NH)NH.sub.2                                                                         Me       H        Ph           OH, OH                               166                                                                               SC(NH)NH.sub.2                                                                         H        OMe      Ph           OH, OH                               167                                                                               CH.sub.2 NH.sub.2                                                                      H        H        Ph           OH, OH                               168                                                                               CH.sub.2 NH.sub.2                                                                      H        Ph       H            OH, OH                               169                                                                               CH.sub.2 NH.sub.2                                                                      H        OPh      H            OH, OH                               170                                                                               CH.sub.2 NH.sub.2                                                                      COPh     H        H            OH, OH                               171                                                                               CH.sub.2 NH.sub.2                                                                      H        COPh     H            OH, OH                               172                                                                               CH.sub.2 NH.sub.2                                                                      H        H        COPh         OH, OH                               173                                                                               CH.sub.2 NH.sub.2                                                                      H        NHCbz    H            OH, OH                               174                                                                               CH.sub.2 NH.sub.2                                                                      H        NMeCbz   H            OH, OH                               175                                                                               CH.sub.2 NH.sub.2                                                                      H        H        Et           OH, OH                               176                                                                               CH.sub.2 NH.sub.2                                                                      H        H        n-Pr         OH, OH                               177                                                                               CH.sub.2 NH.sub.2                                                                      H        H        i-Pr         OH, OH                               178                                                                               CH.sub.2 NH.sub.2                                                                      H        H        n-Bu         OH, OH                               179                                                                               CH.sub.2 NH.sub.2                                                                      H        H        t-Bu         OH, OH                               180                                                                               CH.sub.2 NH.sub.2                                                                      H        H        n-hexyl      OH, OH                               181                                                                               CH.sub.2 NH.sub.2                                                                      H        H        cyclohexyl   OH, OH                               182                                                                               CH.sub.2 NH.sub.2                                                                      NHCOCH.sub.2 CH.sub.2 Ph                                                                H        H            OH, OH                               183                                                                               CH.sub.2 NH.sub.2                                                                      H        H        O-n-Bu       OH, OH                               184                                                                               CH.sub.2 NH.sub.2                                                                      H        H        NHCOcyclopropyl                                                                             OH, OH                               185                                                                               CH.sub.2 NH.sub.2                                                                      H        H        NHCOcyclohexyl                                                                              OH, OH                               186                                                                               CH.sub.2 NH.sub.2                                                                      H        H        NHCO(4-C.sub.6 H.sub.4 OMe)                                                                 OH, OH                               187                                                                               CH.sub.2 NH.sub.2                                                                      H        H        4-C.sub.6 H.sub.4 OMe                                                                       OH, OH                               188                                                                               CH.sub.2 NH.sub.2                                                                      CO.sub.2 CH.sub.2 (2-C.sub.6 H.sub.4 Ph)                                                H        H            OH, OH                               189                                                                               CH.sub.2 NH.sub.2                                                                      H        H        1-naphthyl   OH, OH                               190                                                                               CH.sub.2 NH.sub.2                                                                      H        H        4-C.sub.6 H.sub.4 CO.sub.2 H                                                                OH, OH                               191                                                                               CH.sub.2 NH.sub.2                                                                      H        NHCbz    n-Bu         OH, OH                               192                                                                               CH.sub.2 NH.sub.2                                                                      H        NMeCbz   n-Bu         OH, OH                               193                                                                               CH.sub.2 NH.sub.2                                                                      COPh     H        Me           OH, OH                               194                                                                               CH.sub.2 NH.sub.2                                                                      H        H        4-pyridyl    OH, OH                               195                                                                               CH.sub.2 NH.sub.2                                                                      Me       H        4-C.sub.6 H.sub.4 CO.sub.2 H                                                                OH, OH                               196                                                                               CH.sub.2 NH.sub.2                                                                      H        H        4-C.sub.6 H.sub.4 CO.sub.2 Me                                                               OH, OH                               197                                                                               CH.sub.2 NH.sub.2                                                                      Me       H        4-C.sub.6 H.sub.4 CO.sub.2 Me                                                               OH, OH                               198                                                                               CH.sub.2 NH.sub.2                                                                      Me       H        Ph           OH, OH                               199                                                                               NH(CNH)NH.sub.2                                                                        F        H        Ph           (+)-pin                                                                             SS                              200                                                                               NH(CNH)NH.sub.2                                                                        F        H        Ph           OH, OH                               201                                                                               NH(CNH)NH.sub.2                                                                        NH.sub.2 H        Ph           (+)-pin                              202                                                                               NH(CNH)NH.sub.2                                                                        NH.sub.2 H        Ph           OH, OH                               203                                                                               NH(CNH)NH.sub.2                                                                        NO.sub.2 H        Ph           (+)-pin                                                                             TT                              204                                                                               NH(CNH)NH.sub.2                                                                        NO.sub.2 H        Ph           OH, OH                               205                                                                               NH(CNH)NH.sub.2                                                                        OH       H        Ph           (+)-pin                              206                                                                               NH(CNH)NH.sub.2                                                                        OH       H        Ph           OH, OH                               207                                                                               NH(CNH)NH.sub.2                                                                        NHSO.sub.2 CF.sub.3                                                                     H        Ph           (+)-pin                              208                                                                               NH(CNH)NH.sub.2                                                                        NHSO.sub.2 CF.sub.3                                                                     H        Ph           (+)-pin                              209                                                                               NH(CNH)NH.sub.2                                                                        NHSO.sub.2 CH.sub.3                                                                     H        Ph           (+)-pin                              210                                                                               NH(CNH)NH.sub.2                                                                        NHSO.sub.2 CH.sub.3                                                                     H        Ph           (+)-pin                              211                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.2 CN                                                                             H        Ph           (+)-pin                              212                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.2 CN                                                                             H        Ph           OH, OH                               213                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.2 CH.sub.2 CN                                                                    H        Ph           (+)-pin                              214                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.2 CH.sub.2 CN                                                                    H        Ph           OH, OH                               215                                                                               NH(CNH)NH.sub.2                                                                        OCH.sub.2 CN                                                                            H        Ph           (+)-pin                              216                                                                               NH(CNH)NH.sub.2                                                                        OCH.sub.2 CN                                                                            H        Ph           OH, OH                               217                                                                               NH(CNH)NH.sub.2                                                                        SCH.sub.2 CN                                                                            H        Ph           (+)-pin                              218                                                                               NH(CNH)NH.sub.2                                                                        SCH.sub.2 CN                                                                            H        Ph           OH, OH                               219                                                                               NH(CNH)NH.sub.2                                                                        NHCH.sub.2 CN                                                                           H        Ph           (+)-pin                              220                                                                               NH(CNH)NH.sub.2                                                                        NHCH.sub.2 CN                                                                           H        Ph           OH, OH                               221                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.2 OH                                                                             H        Ph           (+)-pin                              222                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.2 OH                                                                             H        Ph           OH, OH                               223                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(t-butyl-NHSO.sub.2)Ph                                                                    (+)-pin                                                                             UU                              224                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(t-butyl-NHSO.sub.2)Ph                                                                    OH, OH                               225                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(ethyl-NHSO.sub.2)Ph                                                                      (+)-pin                              226                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(ethyl-NHSO.sub.2)Ph                                                                      OH, OH                               227                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(H.sub.2 NSO.sub.2)Ph                                                                     (+)-pin                                                                             ZZ                              228                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(H.sub.2 NSO.sub.2)Ph                                                                     OH, OH                               229                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(MeCONHSO.sub.2)Ph                                                                        (+)-pin                              230                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(MeCONHSO.sub.2)Ph                                                                        OH, OH                               231                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(MeOCONHSO.sub.2)Ph                                                                       (+)-pin                                                                             AB                              232                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(MeOCONHSO.sub.2)Ph                                                                       OH, OH                               233                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(NH.sub.2)Ph                                                                              (+)-pin                              234                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(NH.sub.2)Ph                                                                              OH, OH                               235                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(CH.sub.3 SO.sub.2 NH)Ph                                                                  (+)-pin                              236                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(CH.sub.3 SO.sub.2 NH)Ph                                                                  OH, OH                               237                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(CF.sub.3 SO.sub.2 NH)Ph                                                                  (+)-pin                              238                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(CF.sub.3 SO.sub.2 NH)Ph                                                                  OH, OH                               239                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(CN.sub.4 H)Ph                                                                            (+)-pin                              240                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(CN.sub.4 H)Ph                                                                            OH, OH                               241                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(COOH)Ph   (+)-pin                              242                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(COOH)Ph   OH, OH                               243                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        3-(NH.sub.2)Ph                                                                              (+)-pin                              244                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        3-(NH.sub.2)Ph                                                                              OH, OH                               245                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        3-(CH.sub.3 SO.sub.2 NH)Ph                                                                  (+)-pin                              246                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        3-(CH.sub.3 SO.sub.2 NH)Ph                                                                  OH, OH                               247                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 OH       Ph           (+)-pin                              248                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 OH       Ph           OH, OH                               249                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 NH.sub.2 Ph           (+)-pin                              250                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 NH.sub.2 Ph           OH, OH                               251                                                                               NH(CNH)NH.sub.2                                                                        F        H        2-(t-butyl-NHSO.sub.2)Ph                                                                    (+)-pin                              252                                                                               NH(CNH)NH.sub.2                                                                        F        H        2-(t-butyl-NHSO.sub.2)Ph                                                                    OH, OH                               253                                                                               NH(CNH)NH.sub.2                                                                        F        H        2-(ethyl-NHSO.sub.2)Ph                                                                      (+)-pin                              254                                                                               NH(CNH)NH.sub.2                                                                        F        H        2-(ethyl-NHSO.sub.2)Ph                                                                      OH, OH                               255                                                                               NH(CNH)NH.sub.2                                                                        F        H        2-(H.sub.2 NSO.sub.2)Ph                                                                     (+)-pin                              256                                                                               NH(CNH)NH.sub.2                                                                        F        H        2-(H.sub.2 NSO.sub.2)Ph                                                                     OH, OH                               257                                                                               NH(CNH)NH.sub.2                                                                        F        H        2-(MeCONHSO.sub.2)Ph                                                                        (+)-pin                              258                                                                               NH(CNH)NH.sub.2                                                                        F        H        2-(MeCONHSO.sub.2)Ph                                                                        OH, OH                               259                                                                               NH(CNH)NH.sub.2                                                                        F        H        2-(MeOCONHSO.sub.2)Ph                                                                       (+)-pin                              260                                                                               NH(CNH)NH.sub.2                                                                        F        H        2-(MeOCONHSO.sub.2)Ph                                                                       OH, OH                               261                                                                               NH(CNH)NH.sub.2                                                                        H        H        2-(t-butyl-NHSO.sub.2)Ph                                                                    (+)-pin                                                                             AC                              262                                                                               NH(CNH)NH.sub.2                                                                        Cl       H        2-(t-butyl-NHSO.sub.2)Ph                                                                    (+)-pin                                                                             CE                              263                                                                               NH(CNH)NH.sub.2                                                                        H        H        2-(t-butyl-NHSO.sub.2)Ph                                                                    OH, OH                                                                              AD                              264                                                                               NH(CNH)NH.sub.2                                                                        Cl       H        2-(t-butyl-NHSO.sub.2)Ph                                                                    OH, OH                               265                                                                               NH(CNH)NH.sub.2                                                                        Cl       H        2-(ethyl-NHSO.sub.2)Ph                                                                      (+)-pin                              266                                                                               NH(CNH)NH.sub.2                                                                        Cl       H        2-(ethyl-NHSO.sub.2)Ph                                                                      OH, OH                               267                                                                               NH(CNH)NH.sub.2                                                                        Cl       H        2-(H.sub.2 NSO.sub.2)Ph                                                                     (+)-pin                              268                                                                               NH(CNH)NH.sub.2                                                                        Cl       H        2-(H.sub.2 NSO.sub.2)Ph                                                                     OH, OH                               269                                                                               NH(CNH)NH.sub.2                                                                        Cl       H        2-(MeCONHSO.sub.2)Ph                                                                        (+)-pin                              270                                                                               NH(CNH)NH.sub.2                                                                        Cl       H        2-(MeCONHSO.sub.2)Ph                                                                        OH, OH                               271                                                                               NH(CNH)NH.sub.2                                                                        Cl       H        2-(MeOCONHSO.sub.2)Ph                                                                       (+)-pin                              272                                                                               NH(CNH)NH.sub.2                                                                        Cl       H        2-(MeOCONHSO.sub.2)Ph                                                                       OH, OH                               273                                                                               NH(CNH)NH.sub.2                                                                        NHSO.sub.2 CH.sub.3                                                                     H        2-(t-butyl-NHSO.sub.2)Ph                                                                    (+)-pin                              274                                                                               NH(CNH)NH.sub.2                                                                        NHSO.sub.2 CH.sub.3                                                                     H        2-(t-butyl-NHSO.sub.2)Ph                                                                    OH, OH                               275                                                                               NH(CNH)NH.sub.2                                                                        NHSO.sub.2 CH.sub.3                                                                     H        2-(ethyl-NHSO.sub.2)Ph                                                                      (+)-pin                              276                                                                               NH(CNH)NH.sub.2                                                                        NHSO.sub.2 CH.sub.3                                                                     H        2-(ethyl-NHSO.sub.2)Ph                                                                      OH, OH                               277                                                                               NH(CNH)NH.sub.2                                                                        NHSO.sub.2 CH.sub.3                                                                     H        2-(H.sub.2 NSO.sub.2)Ph                                                                     (+)-pin                              278                                                                               NH(CNH)NH.sub.2                                                                        NHSO.sub.2 CH.sub.3                                                                     H        2-(H.sub.2 NSO.sub.2)Ph                                                                     OH, OH                               279                                                                               NH(CNH)NH.sub.2                                                                        NHSO.sub.2 CH.sub.3                                                                     H        2-(MeCONHSO.sub.2)Ph                                                                        (+)-pin                              280                                                                               NH(CNH)NH.sub.2                                                                        NHSO.sub.2 CH.sub.3                                                                     H        2-(MeCONHSO.sub.2)Ph                                                                        OH, OH                               281                                                                               NH(CNH)NH.sub.2                                                                        NHSO.sub.2 CH.sub.3                                                                     H        2-(MeOCONHSO.sub.2)Ph                                                                       (+)-pin                              282                                                                               NH(CNH)NH.sub.2                                                                        NHSO.sub.2 CH.sub.3                                                                     H        2-(MeOCONHSO.sub.2)Ph                                                                       OH, OH                               283                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        3-(t-butylOCONH)Ph                                                                          (+)-pin                                                                             VV                              284                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        3-(t-butylOCONH)Ph                                                                          OH, OH                               285                                                                               NH(CNH)NH.sub.2                                                                        N(Et).sub.2                                                                             H        Ph           (+)-pin                              286                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-((ethyl).sub.2 -NSO.sub.2)Ph                                                              (+)-pin                                                                             CF                              287                                                                               NH(CNH)NH.sub.2                                                                        CH.sub.3 H        2-(n-BuOCONHSO.sub.2)Ph                                                                     (+)-pin                              288                                                                               NH(CNH)NH.sub.2                                                                        NO.sub.2 H        2-(t-butyl-NHSO.sub.2)Ph                                                                    (+)-pin                                                                             CG                              289                                                                               NH(CNH)NH.sub.2                                                                        NO.sub.2 H        2-(t-butyl-NHSO.sub.2)Ph                                                                    OH, OH                               290                                                                               NH(CNH)NH.sub.2                                                                        NO.sub.2 H        2-(ethyl-NHSO.sub.2)Ph                                                                      (+)-pin                              291                                                                               NH(CNH)NH.sub.2                                                                        NO.sub.2 H        2-(ethyl-NHSO.sub.2)Ph                                                                      OH, OH                               292                                                                               NH(CNH)NH.sub.2                                                                        NO.sub.2 H        2-(H.sub.2 NSO.sub.2)Ph                                                                     (+)-pin                              293                                                                               NH(CNH)NH.sub.2                                                                        NO.sub.2 H        2-(H.sub.2 NSO.sub.2)Ph                                                                     OH, OH                               294                                                                               NH(CNH)NH.sub.2                                                                        NO.sub.2 H        2-(MeCONHSO.sub.2)Ph                                                                        (+)-pin                              295                                                                               NH(CNH)NH.sub.2                                                                        NO.sub.2 H        2-(MeCONHSO.sub.2)Ph                                                                        OH, OH                               296                                                                               NH(CNH)NH.sub.2                                                                        NO.sub.2 H        2-(MeOCONHSO.sub.2)Ph                                                                       (+)-pin                              297                                                                               NH(CNH)NH.sub.2                                                                        NO.sub.2 H        2-(MeOCONHSO.sub.2)Ph                                                                       OH, OH                               298                                                                               NH(CNH)NH.sub.2                                                                        H        NO.sub.2 Ph           (+)-pin                                                                             AE                              299                                                                               NH(CNH)NH.sub.2                                                                        H        NH.sub.2 Ph           (+)-pin                                                                             AF                              300                                                                               NH(CNH)NH.sub.2                                                                        H        NO.sub.2 Ph           OH, OH                               301                                                                               NH(CNH)NH.sub.2                                                                        H        NH.sub.2 Ph           OH, OH                               302                                                                               NH(CNH)H                                                                               H        H        2-(t-butyl-NHSO.sub.2)Ph                                                                    (+)-pin                                                                             CH                              303                                                                               NH(CNH)NH.sub.2                                                                        2-NHBOC  H        Ph           (+)-pin                                                                             CI                              304                                                                               NH(CNH)NH.sub.2                                                                        2-NO.sub.2                                                                              H        Ph           (+)-pin                                                                             CJ                              305                                                                               OCH.sub.3                                                                              2-Me     H        2-(H.sub.2 NSO.sub.2)Ph                                                                     (+)-pin                                                                             CK                              306                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-thiophen-2-yl                                                                             (+)-pin                              307                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-thiophen-3-yl                                                                             (+)-pin                              308                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-thiophen-2-yl                                                                         H            (+)-pin                              309                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-thiophen-3-yl                                                                         H            (+)-pin                              310                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-furan-2-yl (+)-pin                              311                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-furan-3-yl (+)-pin                              312                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-furan-2-yl                                                                            H            (+)-pin                              313                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-furan-3-yl                                                                            H            (+)-pin                              314                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-imidazol-2-yl                                                                             (+)-pin                              315                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-imidazol-4-yl                                                                             (+)-pin                              316                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-imidazol-2-yl                                                                         H            (+)-pin                              317                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-imidazol-4-yl                                                                         H            (+)-pin                              318                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-pyrazol-1-yl                                                                              (+)-pin                              319                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-pyrazol-2-yl                                                                              (+)-pin                              320                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-pyrazol-1-yl                                                                          H            (+)-pin                              321                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-pyrazol-2-yl                                                                          H            (+)-pin                              322                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-pyrrol-1-yl                                                                               (+)-pin                              323                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-pyrrol-2-yl                                                                               (+)-pin                              324                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-pyrrol-1-yl                                                                           H            (+)-pin                              325                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-pyrrol-2-yl                                                                           H            (+)-pin                              326                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-(1,2,4-triazol-1-yl)                                                                      (+)-pin                              327                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-(1,2,4-triazol-2-yl)                                                                      (+)-pin                              328                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-(1,2,4-triazol-1-yl)                                                                  H            (+)-pin                              329                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-(1,2,4-triazol-1-yl)                                                                  H            (+)-pin                              330                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-(1,2,3-triazol-1-yl)                                                                      (+)-pin                              331                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-(1,2,3-triazol-4-yl)                                                                      (+)-pin                              332                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-(1,2,3-triazol-1-yl)                                                                  H            (+)-pin                              333                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-(1,2,3-triazol-4-yl)                                                                  H            (+)-pin                              334                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-tetrazol-1-yl                                                                             (+)-pin                              335                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-tetrazol-5-yl                                                                             (+)-pin                              336                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-tetrazol-1-yl                                                                         H            (+)-pin                              337                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-tetrazol-5-yl                                                                         H            (+)-pin                              338                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-oxazol-2-yl                                                                               (+)-pin                              339                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-oxazol-4-yl                                                                               (+)-pin                              340                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-oxazol-5-yl                                                                               (+)-pin                              341                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-oxazol-2-yl                                                                           H            (+)-pin                              342                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-oxazol-4-yl                                                                           H            (+)-pin                              343                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-oxazol-5-yl                                                                           H            (+)-pin                              344                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-thiazol-2-yl                                                                              (+)-pin                              345                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-thiazol-4-yl                                                                              (+)-pin                              346                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-thiazol-5-yl                                                                              (+)-pin                              347                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-thiazol-2-yl                                                                          H            (+)-pin                              348                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-thiazol-4-yl                                                                          H            (+)-pin                              349                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-thiazol-5-yl                                                                          H            (+)-pin                              350                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-pyridin-2-yl                                                                              (+)-pin                              351                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-pyridin-3-yl                                                                              (+)-pin                              352                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-pyridin-2-yl                                                                          H            (+)-pin                              353                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-pyridin-3-yl                                                                          H            (+)-pin                              354                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-pyrimidin-2-yl                                                                            (+)-pin                              355                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-pyrimidin-4-yl                                                                            (+)-pin                              356                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 H        4-pyrimidin-5-yl                                                                            (+)-pin                              357                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-pyrimidin-2-yl                                                                        H            (+)-pin                              358                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-pyrimidin-4-yl                                                                        H            (+)-pin                              359                                                                               CH.sub.2 NH.sub.2                                                                      CH.sub.3 3-pyrimidin-5-yl                                                                        H            (+)-pin                              __________________________________________________________________________      (+)-pin indicates (+)pinanediol                                                A: MS (M + H).sup.+ = 489;                                                     B: MS (DCINH.sub.3), 505 (M + H).sup.+.                                        C: MS (M + H).sup.+ = 490.                                                     D: MS (M + H).sup.+ = 506;                                                     E: mp 145-150° C.; MS (DCINH.sub.3), Calc: 506, Found: 506.             F: MS (DCINH.sub.3), 522 (M + H).sup.+.                                        G: HRMS (DCINH.sub.3), Calc: 534.2597, Found: 534.2609.                        H: HRMS (DCINH.sub.3), Calc: 534.2597, Found: 534.2605.                        I: HRMS (DCINH.sub.3), Calc: 534.2597, Found: 534.2609.                        J:  a!.sub.D = -14,85° (c = 0.606, MeOH); MS (CINH.sub.3), m/e (%)      537.2 (10.2, M + HH.sub.2 NCN).sup.+), 429.0 (42.8), 277.0 (100); Anal.        Calcd for C.sub.30 H.sub.40 BBrN.sub.4 O.sub.5 S: C, 54.64; H, 6.11; N,        8.50; B, 1.64. Found: C, 54.52; H, 6.16; N, 8.45; B, 1.60.                     K:  a!.sub.D = -15.07° (c = 0.604, MeOH); MS (CINH.sub.3), m/e (%)      593.2 (1.2, (M + H).sup.+), 568.3 (22, (M + NH.sub.4 H.sub.2 NCN).sup.+),      551.3 (100, (M + HH.sub.2 NCN).sup.+); Anal. Calcd for C.sub.31 H.sub.42       BBrN.sub.4 O.sub.5 S: C, 55.29; H, 6.29; N, 8.32; B, 1.61. Found: C,           55.15; H, 6.21; N, 8.22; B, 1.47.                                              L:  a!.sub.D = -14.12° (c = 0.602, MeOH); MS (DCINH.sub.3), m/e (%      458 (100, (M + H).sup.+); Anal. Calcd for C.sub.24 H.sub.37 BBrN.sub.3         O.sub.3 S: C, 53.54; H, 6.93; N, 7.81; B, 2.01. Found: C, 53.75; H, 6.98;      N, 7.74; B, 1.97.                                                              M:  a!.sub.D = -14.21° (c = 0.556, MeOH); MS (CINH.sub.3), m/e (%)      472.2 (13.5, (M + H).sup.+), 430.2 (100, (M + HH.sub.2 NCN).sup.+), 278.0      (61.9); Anal. Calcd for C.sub.25 H.sub.39 BBrN.sub.3 O.sub.3 S: C, 54.36;      H, 7.12; N, 7,61; B, 1.96. Found: C, 54.50; H, 7.18; N, 7.83; B, 1.73.         N:  a!.sub.D = -13.79° (c = 0.602, MeOH); MS (DCINH.sub.3), m/e (%      472 (100, (M + H).sup.+), 430 (37, (M + HH.sub.2 NCN).sup.+); Anal. Calcd      for C.sub.25 H.sub.39 BBrN.sub.3 O.sub.3 S: C, 54.36; H, 7.12; N, 7.61; B      1.96. Found: C, 54.64; H, 7.17; N, 7.50; B, 1.74.                              O:  a .sub.D = -13.19° (c = 0.364, MeOH); MS (CINH.sub.3), m/e (%)      486.2 (3.3, (M + H).sup.+), 444.2 (87.1, (M + HH.sub.2 NCN).sup.+), 292.0      (100); Anal. Calcd for C.sub.26 H.sub.41 BBrN.sub.3 O.sub.3 S: C, 55.13;       H, 7.30; N, 7.42; B, 1.91. Found: C, 54.99; H, 7,22; N, 7.29; B, 2.07.         P:  a!.sub.D = -12.71° (c = 0.598, MeOH); MS (DCINH.sub.3), m/e (%      486 (100, (M + H).sup.+), 444 (16, (M + HH.sub.2 NCN).sup.+); Anal. Calcd      for C.sub.26 H.sub.41 BBrN.sub.3 O.sub.3 S: C, 55.13; H, 7.30; N, 7.42; B      1.91. Found: C, 55.09; H, 7.45; N, 7.40; B, 1.67.                              Q: MS (DCIAB,4 NH.sub.3), m/e (%) 514 (100, (M + H).sup.+), 472 (16, (M +      HH.sub.2 NCN).sup.+); Anal. Calcd for C.sub.28 H.sub.45 BBrN.sub.3 O.sub.      S: C, 56.57; H, 7.63; N, 7.07; B, 1.82. Found: C, 56.19; H, 7.53; N, 6.97      B, 1.99.                                                                       R:  a!.sub.D = -12.70° (c = 0.530, MeOH); MS (DCINH.sub.3), m/e (%      512 (100, (M + H).sup.+), 470 (40, (M + HH.sub.2 NCN).sup.+); Anal. Calcd      for C.sub.28 H.sub.43 BBrN.sub.3 O.sub.3 S: C, 56.77; H, 7.32; N, 7.09; B      1.82. Found: C, 56.49; H, 7.38; N, 6.96; B, 1.75.                              S: HRMS (DCINH.sub.3), Calc: 577.3019, Found: 577.3025.                        T:  a!.sub.D = -8.31° (c = 0.614, MeOH); MS (DCINH.sub.3), m/e (%)      502 (100, (M + H).sup.+), 460 (28, (M + HH.sub.2 NCN).sup.+); Anal. Calcd      for C.sub.26 H.sub.41 BBrN.sub.3 O.sub.4 S: C, 53.62; H, 7.10; N, 7.21; B      1.86. Found: C, 53.61; H, 7.09; N, 7.20; B, 1.78.                              U: HRMS (DCINH.sub.3), Calc: 513.2707, Found: 513.2702.                        V: HRMS (DCINH.sub.3), Calc: 555.3165, Found: 555.3176.                        W: HRMS (DCINH.sub.3), Calc: 579.2812, Found: 579.2801.                        X: HRMS (DCINH.sub.3), Calc: 450.2962, Found: 450.2958.                        Y: HRMS (DCINH.sub.3), Calc: 640.3019, Found: 640.3022.                        Z:  a!.sub.D = -8.80° (c = 0.602, MeOH); MS (CINH.sub.3), m/e (%)       593.2 (1.3, (M + H).sup.+), 485.2 (42.7), 333.0 (100); Anal. Calcd for         C.sub.34 H.sub.48 BBrN.sub.4 O.sub.5 S: C, 57.07; H, 6.76; N, 7.83; B,         1.51. Found: C, 57.17; H, 6.84; N, 7.76; B, 1.41.                              AA: MS (CINH.sub.3), m/e (%) 649.4 (1.9, (M + H).sup.+), 624.4 (31, (M +       NH.sub.4 H.sub.2 NCN).sup.+), 607.2 (100, (M + HH.sub.2 NCN).sup.+), 455.      (39), 444.0 (29.8); Anal. Calcd for C.sub.35 H.sub.50 BBrN.sub.4 O.sub.5       S: C, 57.62; H, 6.91; N, 7.68; B, 1.48. Found: C, 57.37; H, 6.86; N, 7.64      B, 1.40.                                                                       BB: HRMS (DCINH.sub.3), Calc: 520.2805, Found: 520.2796.                       SS. MS (DCINH.sub.3), Calc: 507, Found: 507.                                   TT. MS (DCINH.sub.3), Calc: 534, Found: 534.                                   UU. MS (DCINH.sub.3), Calc: 638, Found: 638.                                   VV. MS (DCINH.sub.3), Calc: 618, Found: 618.                                   XX. MS (DCINH.sub.3), Calc: 489, Found: 489.                                   YY. MS (DCINH.sub.3), Calc: 461, Found: 461.                                   ZZ. MS (DCINH.sub.3), Calc: 582, Found: 582.                                   AB. MS (DCINH.sub.3), Calc: 641, Found: 641.                                   AC. MS (DCINH.sub.3), Calc: 625, Found: 625.                                   AD. MS (DCINH.sub.3), Calc: 490, Found: 490.                                   AE. MS (DCINH.sub.3), Calc: 534, Found: 534.                                   AF. MS (DCINH.sub.3), Calc: 504, Found: 504.                                   CB. MS (M + H).sup.+, Calc: 503.32, Found: 503.32.                             CD. MS (M + H).sup.+, Calc: , Found: .(WITYAK)                                 CE. MS (M + H).sup.+, Calc: 658, Found: 658.                                   CF. MS (M + H).sup.+, Calc: 638, Found: 638.                                   CG. MS (M + H).sup.+, Calc: 669, Found: 669.                                   CH. MS (M + H).sup.+, Calc: 609, Found: 609.                                   CI. MS (M + H).sup.+, Calc: 604, Found: 604.                                   CJ. MS (M + H).sup.+, Calc: 641, Found: 641.                                   CK. MS (M + H).sup.+, Calc: 555, Found: 555.                             

                  TABLE 2                                                          ______________________________________                                          ##STR97##                                                                     Ex      X           Y       Y.sup.1, Y.sup.2                                                                      Phys Data                                   ______________________________________                                         365     CH.sub.2 NH.sub.2                                                                          CO      (+)-pin                                            366     CH.sub.2 NH.sub.2                                                                          SO.sub.2                                                                               (+)-pin                                            367     NHC(NH)NH.sub.2                                                                            CO      (+)-pin                                            368     NHC(NH)NH.sub.2                                                                            SO.sub.2                                                                               (+)-pin                                            369     SC(NH)NH.sub.2                                                                             CO      (+)-pin                                                                               CC                                          370     SC(NH)NH.sub.2                                                                             SO.sub.2                                                                               (+)-pin                                                                               DD                                          371     CH.sub.2 NH.sub.2                                                                          CO      OH, OH                                             372     CH.sub.2 NH.sub.2                                                                          SO.sub.2                                                                               OH, OH                                             373     NHC(NH)NH.sub.2                                                                            CO      OH, OH                                             374     NHC(NH)NH.sub.2                                                                            SO.sub.2                                                                               OH, OH                                             375     SC(NH)NH.sub.2                                                                             CO      OH, OH                                             376     SC(NH)NH.sub.2                                                                             SO.sub.2                                                                               OH, OH                                             ______________________________________                                          CC: HRMS (DCINH.sub.3), Calc: 560.2390, Found: 560.2407.                       DD: HRMS (DCINH.sub.3), Calc: 596.2060, Found: 596.2055.                 

                  TABLE 3                                                          ______________________________________                                          ##STR98##                                                                     Ex      X          t        Y.sup.1, Y.sup.2                                                                      Phys Data                                   ______________________________________                                         382     NH.sub.2   2        (+)-pin                                            383     SC(NH)NH.sub.2                                                                            2        (+)-pin                                                                               EE                                          384     SC(NH)NH.sub.2                                                                            1        (+)-pin                                                                               FF                                          385     NHC(NH)NH.sub.2                                                                           2        (+)-pin                                            386     NHC(NH)NH.sub.2                                                                           1        (+)-pin                                            387     NH.sub.2   2        OH, OH                                             388     SC(NH)NH.sub.2                                                                            2        OH, OH                                             389     SC(NH)NH.sub.2                                                                            1        OH, OH                                             390     NHC(NH)NH.sub.2                                                                           2        OH, OH                                             391     NHC(NH)NH.sub.2                                                                           1        OH, OH                                             ______________________________________                                          EE: HRMS (DCINH.sub.3), Calc: 546.2597, Found: 546.2604.                       FF: HRMS (DCINH.sub.3), Calc: 534.2597, Found: 534.2609.                 

                  TABLE 4                                                          ______________________________________                                          ##STR99##                                                                     Ex        X            Y.sup.1, Y.sup.2                                                                        Phys Data                                      ______________________________________                                         397       CH.sub.2 NH.sub.2                                                                           (+)-pin                                                 398       NHC(NH)NH.sub.2                                                                             (+)-pin                                                 399       SC(NH)NH.sub.2                                                                              (+)-pin  CG                                             400       CH.sub.2 NH.sub.2                                                                           OH, OH                                                  401       NHC(NH)NH.sub.2                                                                             OH, OH                                                  402       SC(NH)NH.sub.2                                                                              OH, OH                                                  ______________________________________                                          GG: HRMS (DCINH.sub.3), Calc: 532.2441, Found: 532.2445.                 

                  TABLE 5                                                          ______________________________________                                          ##STR100##                                                                    Ex        X            Y.sup.1, Y.sup.2                                                                        Phys Data                                      ______________________________________                                         403       CH.sub.2 NH.sub.2                                                                           (+)-pin                                                 404       NHC(NH)NH.sub.2                                                                             (+)-pin                                                 405       SC(NH)NH.sub.2                                                                              (+)-pin  HH                                             406       CH.sub.2 NH.sub.2                                                                           OH, OH                                                  407       NHC(NH)NH.sub.2                                                                             OH, OH                                                  408       SC(NH)NH.sub.2                                                                              OH, OH                                                  ______________________________________                                          HH: HRMS (DCINH.sub.3), Calc: 532.2441, Found: 532.2452.                 

                  TABLE 6                                                          ______________________________________                                          ##STR101##                                                                    Ex        X            Y.sup.1, Y.sup.2                                                                        Phys Data                                      ______________________________________                                         436       NHC(NH)NH.sub.2                                                                             (+)-pin                                                 437       SC(NH)NH.sub.2                                                                              (+)-pin  II                                             438       CH.sub.2 NH.sub.2                                                                           (+)-pin                                                 439       NHC(NH)NH.sub.2                                                                             OH, OH                                                  440       SC(NH)NH.sub.2                                                                              OH, OH                                                  441       CH.sub.2 NH.sub.2                                                                           OH, OH                                                  ______________________________________                                          II: HRMS (DCINH.sub.3), Calc: 480.2493, Found: 480.2492.                 

                  TABLE 7                                                          ______________________________________                                          ##STR102##                                                                    Ex      X          Y        Y.sup.1, Y.sup.2                                                                      Phys Data                                   ______________________________________                                         447     NHC(NH)NH.sub.2                                                                           O        (+)-pin                                                                               WW                                          448     SC(NH)NH.sub.2                                                                            O        (+)-pin                                                                               JJ                                          449     CH.sub.2 NH.sub.2                                                                         O        (+)-pin                                            450     NHC(NH)NH.sub.2                                                                           S        (+)-pin                                            451     SC(NH)NH.sub.2                                                                            S        (+)-pin                                            452     CH.sub.2 NH.sub.2                                                                         S        (+)-pin                                            453     NHC(NH)NH.sub.2                                                                           O        OH, OH                                             454     SC(NH)NH.sub.2                                                                            O        OH, OH                                             455     CH.sub.2 NH.sub.2                                                                         O        OH, OH                                             456     NHC(NH)NH.sub.2                                                                           S        OH, OH                                             457     SC(NH)NH.sub.2                                                                            S        OH, OH                                             458     CH.sub.2 NH.sub.2                                                                         S        OH, OH                                             ______________________________________                                          JJ: HRMS (DCINH.sub.3), Calc: 496.2441, Found: 496.2449.                       WW. MS (DCINH.sub.3), Calc: 345, Found: 345.                             

                  TABLE 8                                                          ______________________________________                                          ##STR103##                                                                    Ex    X           R.sup.B R.sup.C                                                                             Y.sup.1, Y.sup.2                                                                       Phys Data                               ______________________________________                                         464   NHC(NH)NH.sub.2                                                                            H       Ph   (+)-pin                                         465   NHC(NH)NH.sub.2                                                                            OBn     H    (+)-pin                                         466   SC(NH)NH.sub.2                                                                             H       Ph   (+)-pin KK                                      467   SC(NH)NH.sub.2                                                                             OBn     H    (+)-pin LL                                      468   CH.sub.2 NH.sub.2                                                                          H       Ph   (+)-pin CL                                      469   CH.sub.2 NH.sub.2                                                                          OBn     H    (+)-pin                                         470   NHC(NH)NH.sub.2                                                                            H       Ph   OH, OH                                          471   NHC(NH)NH.sub.2                                                                            OBn     H    OH, OH                                          472   SC(NH)NH.sub.2                                                                             H       Ph   OH, OH                                          473   SC(NH)NH.sub.2                                                                             OBn     H    OH, OH                                          474   CH.sub.2 NH.sub.2                                                                          H       Ph   OH, OH  CM                                      475   CH.sub.2 NH.sub.2                                                                          OBn     H    OH, OH                                          ______________________________________                                          KK: HRMS (DCINH.sub.3), Calc: 507.2601, Found: 507.2592.                       LL: HRMS (DCINH.sub.3), Calc: 537.2667, Found: 537.2685.                       CL: Anal. Calc'd. for C.sub.27 H.sub.36 BN.sub.3                               O.sub.3.(HCl).sub.1.7.(H.sub.2 O).sub.2.2 : C, 57.60; H, 7.54; Cl, 10.70;      N, 7.46. Found: C, 57.40; H, 7.23; Cl, 10.78; N, 7.53. MS (M + H).sup.+ :      calc. 462, Found 462.                                                          CM: MS (M + H).sup.+ : Calc: 328, Found: 328.                            

                  TABLE 9                                                          ______________________________________                                          ##STR104##                                                                    Ex        X            Y.sup.1, Y.sup.2                                                                        Phys Data                                      ______________________________________                                         476       NHC(NH)NH.sub.2                                                                             (+)-pin                                                 477       SC(NH)NH.sub.2                                                                              (+)-pin  MM                                             478       CH.sub.2 NH.sub.2                                                                           (+)-pin                                                 479       NHC(NH)NH.sub.2                                                                             OH, OH                                                  480       SC(NH)NH.sub.2                                                                              OH, OH                                                  481       CH.sub.2 NH.sub.2                                                                           OH, OH                                                  ______________________________________                                          MM: HRMS (DCINH.sub.3), Calc: 498.2233, Found: 498.2231.                 

                  TABLE 10                                                         ______________________________________                                          ##STR105##                                                                    Ex    X          W.sup.1                                                                               W.sup.2                                                                             R.sup.3                                                                             Y.sup.1, Y.sup.2                                                                      Phys Data                             ______________________________________                                         482   NHC(NH)NH.sub.2                                                                           N      CH   H    (+)-pin                                      483   SC(NH)NH.sub.2                                                                            N      CH   H    (+)-pin                                                                               NN                                    484   CH.sub.2 NH.sub.2                                                                         N      CH   H    (+)-pin                                      485   NHC(NH)NH.sub.2                                                                           CH     N    Ph   (+)-pin                                      486   SC(NH)NH.sub.2                                                                            CH     N    Ph   (+)-pin                                                                               OO                                    487   CH.sub.2 NH.sub.2                                                                         CH     N    Ph   (+)-pin                                      488   NHC(NH)NH.sub.2                                                                           N      CH   H    OH, OH                                       489   SC(NH)NH.sub.2                                                                            N      CH   H    OH, OH                                       490   CH.sub.2 NH.sub.2                                                                         N      CH   H    OH, OH                                       491   NHC(NH)NH.sub.2                                                                           CH     N    Ph   OH, OH                                       492   SC(NH)NH.sub.2                                                                            CH     N    Ph   OH, OH                                       493   CH.sub.2 NH.sub.2                                                                         CH     N    Ph   OH, OH                                       ______________________________________                                          NN: HRMS (DCINH.sub.3), Calc: 481.2445, Found: 481.2442.                       OO: HRMS (DCINH.sub.3), Calc: 557.2758, Found: 557.2754.                 

                  TABLE 11                                                         ______________________________________                                          ##STR106##                                                                    Ex        X            Y.sup.1, Y.sup.2                                                                        Phys Data                                      ______________________________________                                         499       NHC(NH)NH.sub.2                                                                             (+)-pin                                                 500       SC(NH)NH.sub.2                                                                              (+)-pin  PP                                             501       CH.sub.2 NH.sub.2                                                                           (+)-pin                                                 502       NHC(NH)NH.sub.2                                                                             OH, OH                                                  503       SC(NH)NH.sub.2                                                                              OH, OH                                                  504       CH.sub.2 NH.sub.2                                                                           OH, OH                                                  ______________________________________                                          PP: HRMS (DCINH.sub.3), Calc: 5481.2445, Found: 481.2440.                

                  TABLE 12                                                         ______________________________________                                          ##STR107##                                                                    Ex      X         R.sup.3  Y.sup.1, Y.sup.2                                                                      Phys Data                                    ______________________________________                                         510     SC(NH)NH.sub.2                                                                           H        (+)-pin                                                                               QQ                                           ______________________________________                                          QQ: HRNS (NH.sub.3 CI/DEP), Calc: 503.3193, Found: 503.3199.             

                  TABLE 13                                                         ______________________________________                                          ##STR108##                                                                                                                Phys                               Ex   m, X       R.sup.A R.sup.B                                                                               R.sup.C                                                                              Y.sup.1, Y.sup.2                                                                      Data                               ______________________________________                                         516  2,         H       NHCO   H     (+)-pin                                                                               RR                                      SC(NH)NH.sub.2     (CH.sub.2).sub.2 Ph                                    517  2,         H       Ph     H     (+)-pin                                        SC (NH) NH.sub.2                                                          518  2,         H       OPh    Ph    (+)-pin                                        SC(NH)NH.sub.2                                                            519  1,         H       H      4-    (+)-pin                                        SC(NH)NH.sub.2            pyridyl                                         520  1,         COPh    H      H     (+)-pin                                        NHC(NH)NH.sub.2                                                           521  3,         H       COPh   H     (+)-pin                                        NHC(NH)NH.sub.2                                                           522  3,         H       H      COPh  (+)-pin                                        NHC(NH)NH.sub.2                                                           ______________________________________                                          RR: HRMS (DCINH.sub.3), Calc: 605.333, Found: 605.3325.                  

                                      TABLE 14                                     __________________________________________________________________________      ##STR109##                                                                                                              Phys.                                Ex X           m R.sup.13                                                                               R.sup.14 Y.sup.1 Y.sup.2                                                                        Data                                 __________________________________________________________________________      528                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      H        (+)-pin                                       529                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      Methyl   (+)-pin                                       530                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      Ethyl    (+)-pin                                       531                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      n-Propyl (+)-pin                                       532                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      n-Butyl  (+)-pin                                       533                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 SCH.sub.3                                                                      (+)-pin                                       534                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                       535                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                       536                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                       537                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                       538                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                       539                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CN                                                                             (+)-pin                                       540                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                       541                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                       542                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CF.sub.3 (+)-pin                                       543                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CF.sub.2 CF.sub.3                                                                       (+)-pin                                       544                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                       545                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                       546                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      F.sub.5 -Ph                                                                             (+)-pin                                       547                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                       548                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                       549                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                       550                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                       551                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                       552                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                       553                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 NO.sub.2                                                                       (+)-pin                                       554                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                       555                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                       556                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 OH                                                                             (+)-pin                                       557                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.2 OH                                                                     (+)-pin                                       558                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.3 OH                                                                     (+)-pin                                       559                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                       560                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                       561                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                       562                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      Ph       (+)-pin                                       563                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      PhCH.sub.2                                                                              (+)-pin AG                                    564                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      Ph(CH.sub.2).sub.2                                                                      (+)-pin                                       565                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      3-NO.sub.2 -Ph                                                                          (+)-pin                                       566                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      4-NO.sub.2 -Ph                                                                          (+)-pin                                       567                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      3-CO.sub.2 H-Ph                                                                         (+)-pin                                       568                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      4-CO.sub.2 H-Ph                                                                         (+)-pin                                       569                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      3-CN.sub.4 H-Ph                                                                         (+)-pin                                       570                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      4-CN.sub.4 H-Ph                                                                         (+)-pin                                       571                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                       572                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                       573                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      H        (+)-pin                                       574                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      Methyl   (+)-pin                                       575                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      Ethyl    (+)-pin                                       576                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      n-Propyl (+)-pin                                       577                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      n-Butyl  (+)-pin                                       578                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 SCH.sub.3                                                                      (+)-pin                                       579                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                       580                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                       581                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                       582                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                       583                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                       584                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CN                                                                             (+)-pin                                       585                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                       586                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                       587                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CF.sub.3 (+)-pin                                       588                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CF.sub.2 CF.sub.3                                                                       (+)-pin                                       589                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                       590                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                       591                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      F.sub.5 -Ph                                                                             (+)-pin                                       592                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                       593                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                       594                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                       595                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                       596                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                       597                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                       598                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 NO.sub.2                                                                       (+)-pin                                       599                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                       600                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                       601                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 OH                                                                             (+)-pin                                       602                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.2 OH                                                                     (+)-pin                                       603                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.3 OH                                                                     (+)-pin                                       604                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                       605                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                       606                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                       607                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      Ph       (+)-pin                                       609                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      3-NO.sub.2 -Ph                                                                          (+)-pin                                       610                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      4-NO.sub.2 -Ph                                                                          (+)-pin                                       611                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      3-CO.sub.2 H-Ph                                                                         (+)-pin                                       612                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      4-CO.sub.2 H-Ph                                                                         (+)-pin                                       613                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      3-CN.sub.4 H-Ph                                                                         (+)-pin                                       614                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      4-CN.sub.4 H-Ph                                                                         (+)-pin                                       615                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                       616                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                       617                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      H        OH, OH                                        618                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      Methyl   OH, OH                                        619                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      Ethyl    OH, OH                                        620                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      n-Propyl OH, OH                                        621                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      n-Butyl  OH, OH                                        622                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 SCH.sub.3                                                                      OH, OH                                        623                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                        624                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                        625                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                        626                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                        627                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                        628                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CN                                                                             OH, OH                                        629                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                        630                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                        631                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CF.sub.3 OH, OH                                        632                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CF.sub.2 CF.sub.3                                                                       OH, OH                                        633                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                        634                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                        635                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      F.sub.5 -Ph                                                                             OH, OH                                        636                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CO.sub.2 H                                                                     OH, OH                                        637                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                        638                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                        639                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CN.sub.4 H                                                                     OH, OH                                        640                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                        641                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                        642                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 NO.sub.2                                                                       OH, OH                                        643                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                        644                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                        645                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 OH                                                                             OH, OH                                        646                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.2 OH                                                                     OH, OH                                        647                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.3 OH                                                                     OH, OH                                        648                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                        649                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                        650                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                        651                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      Ph       OH, OH                                        652                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      PhCH.sub.2                                                                              OH, OH  AH                                    653                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      Ph(CH.sub.2).sub.2                                                                      OH, OH                                        654                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      3-NO.sub.2 -Ph                                                                          OH, OH                                        655                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      4-NO.sub.2 -Ph                                                                          OH, OH                                        656                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      3-CO.sub.2 H-Ph                                                                         OH, OH                                        657                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      4-CO.sub.2 H-Ph                                                                         OH, OH                                        658                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      3-CN.sub.4 H-Ph                                                                         OH, OH                                        659                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      4-CN.sub.4 H-Ph                                                                         OH, OH                                        660                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      3-(HOCH.sub.2)-Ph                                                                       OH, OH                                        661                                                                              CH.sub.2 NH.sub.2                                                                          1 Ph      4-(HOCH.sub.2)-Ph                                                                       OH, OH                                        662                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      H        OH, OH                                        663                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      Methyl   OH, OH                                        664                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      Ethyl    OH, OH                                        665                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      n-Propyl OH, OH                                        666                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      n-Butyl  OH, OH                                        667                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 SCH.sub.3                                                                      OH, OH                                        668                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                        669                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                        670                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                        671                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                        672                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                        673                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CN                                                                             OH, OH                                        674                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                        675                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                        676                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CF.sub.3 OH, OH                                        677                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CF.sub.2 CF.sub.3                                                                       OH, OH                                        678                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                        679                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                        680                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      F.sub.5 -Ph                                                                             OH, OH                                        681                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CO.sub.2 H                                                                     OH, OH                                        682                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                        683                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                        684                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CN.sub.4 H                                                                     OH, OH                                        685                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                        686                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                        687                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 NO.sub.2                                                                       OH, OH                                        688                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                        689                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                        690                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 OH                                                                             OH, OH                                        691                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.2 OH                                                                     OH, OH                                        692                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.3 OH                                                                     OH, OH                                        693                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                        694                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                        695                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                        696                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      Ph       OH, OH                                        697                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      PhCH.sub.2                                                                              OH, OH                                        698                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      Ph(CH.sub.2).sub.2                                                                      OH, OH                                        699                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      3-NO.sub.2 -Ph                                                                          OH, OH                                        700                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      4-NO.sub.2 -Ph                                                                          OH, OH                                        701                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      3-CO.sub.2 H-Ph                                                                         OH, OH                                        702                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      4-CO.sub.2 H-Ph                                                                         OH, OH                                        703                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      3-CN.sub.4 H-Ph                                                                         OH, OH                                        704                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      4-CN.sub.4 H-Ph                                                                         OH, OH                                        705                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      3-(HOCH.sub.2)-Ph                                                                       OH, OH                                        706                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      4-(HOCH.sub.2)-Ph                                                                       OH, OH                                        707                                                                              S(CNH)NH.sub.2                                                                             1 Ph      H        (+)-pin                                       708                                                                              S(CNH)NH.sub.2                                                                             1 Ph      Methyl   (+)-pin                                       709                                                                              S(CNH)NH.sub.2                                                                             1 Ph      Ethyl    (+)-pin                                       710                                                                              S(CNH)NH.sub.2                                                                             1 Ph      n-Propyl (+)-pin                                       711                                                                              S(CNH)NH.sub.2                                                                             1 Ph      n-Butyl  (+)-pin                                       712                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 SCH.sub.3                                                                      (+)-pin                                       713                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                       714                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                       715                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                       716                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                       717                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                       718                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CN                                                                             (+)-pin                                       719                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                       720                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                       721                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CF.sub.3 (+)-pin                                       722                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CF.sub.2 CF.sub.3                                                                       (+)-pin                                       723                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                       724                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                       725                                                                              S(CNH)NH.sub.2                                                                             1 Ph      F.sub.5 -Ph                                                                             (+)-pin                                       726                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                       727                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                       728                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                       729                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                       730                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                       731                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                       732                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 NO.sub.2                                                                       (+)-pin                                       733                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                       734                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                       735                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 OH                                                                             (+)-pin                                       736                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.2 OH                                                                     (+)-pin                                       737                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.3 OH                                                                     (+)-pin                                       738                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                       739                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                       740                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                       741                                                                              S(CNH)NH.sub.2                                                                             1 Ph      Ph       (+)-pin                                       742                                                                              S(CNH)NH.sub.2                                                                             1 Ph      3-NO.sub.2 -Ph                                                                          (+)-pin                                       743                                                                              S(CNH)NH.sub.2                                                                             1 Ph      4-NO.sub.2 -Ph                                                                          (+)-pin                                       744                                                                              S(CNH)NH.sub.2                                                                             1 Ph      3-CO.sub.2 H-Ph                                                                         (+)-pin                                       745                                                                              S(CNH)NH.sub.2                                                                             1 Ph      4-CO.sub.2 H-Ph                                                                         (+)-pin                                       746                                                                              S(CNH)NH.sub.2                                                                             1 Ph      3-CN.sub.4 H-Ph                                                                         (+)-pin                                       747                                                                              S(CNH)NH.sub.2                                                                             1 Ph      4-CN.sub.4 H-Ph                                                                         (+)-pin                                       748                                                                              S(CNH)NH.sub.2                                                                             1 Ph      3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                       749                                                                              S(CNH)NH.sub.2                                                                             1 Ph      4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                       750                                                                              S(CNH)NH.sub.2                                                                             1 Ph      H        OH, OH                                        751                                                                              S(CNH)NH.sub.2                                                                             1 Ph      Methyl   OH, OH                                        752                                                                              S(CNH)NH.sub.2                                                                             1 Ph      Ethyl    OH, OH                                        753                                                                              S(CNH)NH.sub.2                                                                             1 Ph      n-Propyl OH, OH                                        754                                                                              S(CNH)NH.sub.2                                                                             1 Ph      n-Butyl  OH, OH                                        755                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 SCH.sub.3                                                                      OH, OH                                        756                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                        757                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                        758                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                        759                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                        760                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                        761                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CN                                                                             OH, OH                                        762                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                        763                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                        764                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CF.sub.3 OH, OH                                        765                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CF.sub.2 CF.sub.3                                                                       OH, OH                                        766                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                        767                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                        768                                                                              S(CNH)NH.sub.2                                                                             1 Ph      F.sub.5 -Ph                                                                             OH, OH                                        769                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CO.sub.2 H                                                                     OH, OH                                        770                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                        771                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                        772                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CN.sub.4 H                                                                     OH, OH                                        773                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                        774                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                        775                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 NO.sub.2                                                                       OH, OH                                        776                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                        777                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                        778                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 OH                                                                             OH, OH                                        779                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.2 OH                                                                     OH, OH                                        780                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.3 OH                                                                     OH, OH                                        781                                                                              S(CNH)NH.sub.2                                                                             1 Ph      CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                        782                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                        783                                                                              S(CNH)NH.sub.2                                                                             1 Ph      (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                        784                                                                              S(CNH)NH.sub.2                                                                             1 Ph      Ph       OH, OH                                        785                                                                              S(CNH)NH.sub.2                                                                             1 Ph      PhCH.sub.2                                                                              OH, OH                                        786                                                                              S(CNH)NH.sub.2                                                                             1 Ph      Ph(CH.sub.2).sub.2                                                                      OH, OH                                        787                                                                              S(CNH)NH.sub.2                                                                             1 Ph      3-NO.sub.2 -Ph                                                                          OH, OH                                        788                                                                              S(CNH)NH.sub.2                                                                             1 Ph      4-NO.sub.2 -Ph                                                                          OH, OH                                        789                                                                              S(CNH)NH.sub.2                                                                             1 Ph      3-CO.sub.2 H-Ph                                                                         OH, OH                                        790                                                                              S(CNH)NH.sub.2                                                                             1 Ph      4-CO.sub.2 H-Ph                                                                         OH, OH                                        791                                                                              S(CNH)NH.sub.2                                                                             1 Ph      3-CN.sub.4 H-Ph                                                                         OH, OH                                        792                                                                              S(CNH)NH.sub.2                                                                             1 Ph      4-CN.sub.4 H-Ph                                                                         OH, OH                                        793                                                                              S(CNH)NH.sub.2                                                                             1 Ph      3-(HOCH.sub.2)-Ph                                                                       OH, OH                                        794                                                                              S(CNH)NH.sub.2                                                                             1 Ph      4-(HOCH.sub.2)-Ph                                                                       OH, OH                                        795                                                                              CH.sub.2 NH.sub.2                                                                          2 Ph      H        (+)-pin                                       796                                                                              CH.sub.2 NH.sub.2                                                                          2 Ph      H        OH, OH                                        797                                                                              OMe         1 Ph      H        (+)-pin                                       798                                                                              OMe         1 Ph      Methyl   (+)-pin                                       799                                                                              OMe         1 Ph      Ethyl    (+)-pin                                       800                                                                              OMe         1 Ph      n-Propyl (+)-pin                                       801                                                                              OMe         1 Ph      n-Butyl  (+)-pin                                       802                                                                              OMe         1 Ph      CH.sub.2 SCH.sub.3                                                                      (+)-pin                                       803                                                                              OMe         1 Ph      CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                       804                                                                              OMe         1 Ph      CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                       805                                                                              OMe         1 Ph      CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                       806                                                                              OMe         1 Ph      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                       807                                                                              OMe         1 Ph      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                       808                                                                              OMe         1 Ph      CH.sub.2 CN                                                                             (+)-pin                                       809                                                                              OMe         1 Ph      CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                       810                                                                              OMe         1 Ph      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                       811                                                                              OMe         1 Ph      CF.sub.3 (+)-pin                                       812                                                                              OMe         1 Ph      CF.sub.2 CF.sub.3                                                                       (+)-pin                                       813                                                                              OMe         1 Ph      CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                       814                                                                              OMe         1 Ph      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                       815                                                                              OMe         1 Ph      F.sub.5 -Ph                                                                             (+)-pin                                       816                                                                              OMe         1 Ph      CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                       817                                                                              OMe         1 Ph      (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                       818                                                                              OMe         1 Ph      (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                       819                                                                              OMe         1 Ph      CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                       820                                                                              OMe         1 Ph      (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                       821                                                                              OMe         1 Ph      (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                       822                                                                              OMe         1 Ph      CH.sub.2 NO.sub.2                                                                       (+)-pin                                       823                                                                              OMe         1 Ph      (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                       824                                                                              OMe         1 Ph      (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                       825                                                                              OMe         1 Ph      CH.sub.2 OH                                                                             (+)-pin                                       826                                                                              OMe         1 Ph      (CH.sub.2).sub.2 OH                                                                     (+)-pin                                       827                                                                              OMe         1 Ph      (CH.sub.2).sub.3 OH                                                                     (+)-pin                                       828                                                                              OMe         1 Ph      CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                       829                                                                              OMe         1 Ph      (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                       830                                                                              OMe         1 Ph      (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                       831                                                                              OMe         1 Ph      Ph       (+)-pin                                       832                                                                              OMe         1 Ph      PhCH.sub.2                                                                              (+)-pin                                       833                                                                              OMe         1 Ph      Ph(CH.sub.2).sub.2                                                                      (+)-pin                                       834                                                                              OMe         1 Ph      3-NO.sub.2 -Ph                                                                          (+)-pin                                       835                                                                              OMe         1 Ph      4-NO.sub.2 -Ph                                                                          (+)-pin                                       836                                                                              OMe         1 Ph      3-CO.sub.2 H-Ph                                                                         (+)-pin                                       837                                                                              OMe         1 Ph      4-CO.sub.2 H-Ph                                                                         (+)-pin                                       838                                                                              OMe         1 Ph      3-CN.sub.4 H-Ph                                                                         (+)-pin                                       839                                                                              OMe         1 Ph      4-CN.sub.4 H-Ph                                                                         (+)-pin                                       840                                                                              OMe         1 Ph      3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                       841                                                                              OMe         1 Ph      4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                       842                                                                              OMe         1 Ph      H        OH, OH                                        843                                                                              OMe         1 Ph      Methyl   OH, OH                                        844                                                                              OMe         1 Ph      Ethyl    OH, OH                                        845                                                                              OMe         1 Ph      n-Propyl OH, OH                                        846                                                                              OMe         1 Ph      n-Butyl  OH, OH                                        847                                                                              OMe         1 Ph      CH.sub.2 SCH.sub.3                                                                      OH, OH                                        848                                                                              OMe         1 Ph      CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                        849                                                                              OMe         1 Ph      CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                        850                                                                              OMe         1 Ph      CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                        851                                                                              OMe         1 Ph      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                        852                                                                              OMe         1 Ph      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                        853                                                                              OMe         1 Ph      CH.sub.2 CN                                                                             OH, OH                                        854                                                                              OMe         1 Ph      CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                        855                                                                              OMe         1 Ph      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                        856                                                                              OMe         1 Ph      CF.sub.3 OH, OH                                        857                                                                              OMe         1 Ph      CF.sub.2 CF.sub.3                                                                       OH, OH                                        858                                                                              OMe         1 Ph      CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                        859                                                                              OMe         1 Ph      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                        860                                                                              OMe         1 Ph      F.sub.5 -Ph                                                                             OH, OH                                        861                                                                              OMe         1 Ph      CH.sub.2 CO.sub.2 H                                                                     OH, OH                                        862                                                                              OMe         1 Ph      (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                        863                                                                              OMe         1 Ph      (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                        864                                                                              OMe         1 Ph      CH.sub.2 CN.sub.4 H                                                                     OH, OH                                        865                                                                              OMe         1 Ph      (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                        866                                                                              OMe         1 Ph      (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                        867                                                                              OMe         1 Ph      CH.sub.2 NO.sub.2                                                                       OH, OH                                        868                                                                              OMe         1 Ph      (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                        869                                                                              OMe         1 Ph      (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                        870                                                                              OMe         1 Ph      CH.sub.2 OH                                                                             OH, OH                                        871                                                                              OMe         1 Ph      (CH.sub.2).sub.2 OH                                                                     OH, OH                                        872                                                                              OMe         1 Ph      (CH.sub.2).sub.3 OH                                                                     OH, OH                                        873                                                                              OMe         1 Ph      CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                        874                                                                              OMe         1 Ph      (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                        875                                                                              OMe         1 Ph      (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                        876                                                                              OMe         1 Ph      Ph       OH, OH                                        877                                                                              OMe         1 Ph      PhCH.sub.2                                                                              OH, OH                                        878                                                                              OMe         1 Ph      Ph(CH.sub.2).sub.2                                                                      OH, OH                                        879                                                                              OMe         1 Ph      3-NO.sub.2 -Ph                                                                          OH, OH                                        880                                                                              OMe         1 Ph      4-NO.sub.2 -Ph                                                                          OH, OH                                        881                                                                              OMe         1 Ph      3-CO.sub.2 H-Ph                                                                         OH, OH                                        882                                                                              OMe         1 Ph      4-CO.sub.2 H-Ph                                                                         OH, OH                                        883                                                                              OMe         1 Ph      3-CN.sub.4 H-Ph                                                                         OH, OH                                        884                                                                              OMe         1 Ph      4-CN.sub.4 H-Ph                                                                         OH, OH                                        885                                                                              OMe         1 Ph      3-(HOCH.sub.2)-Ph                                                                       OH, OH                                        886                                                                              OMe         1 Ph      4-(HOCH.sub.2)-Ph                                                                       OH, OH                                        887                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             H        (+)-pin AK                                    888                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             Methyl   (+)-pin AL                                    889                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             Ethyl    (+)-pin                                       890                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             n-Propyl (+)-pin AM                                    891                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             n-Butyl  (+)-pin                                       892                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 SCH.sub.3                                                                      (+)-pin AN                                    893                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                       894                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                       895                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                       896                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                       897                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                       898                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin CN                                    899                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                       900                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CF.sub.3 (+)-pin                                       901                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.3                                                                       (+)-pin                                       902                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                       903                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                       904                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             F.sub.5 -Ph                                                                             (+)-pin                                       905                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 H                                                                     (+)-pin AW                                    906                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                       907                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                       908                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                       909                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                       910                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                       911                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                       912                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                       913                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 OH                                                                             (+)-pin AO                                    914                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 OCH.sub.2 Ph                                                                   (+)-pin AP                                    915                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                       916                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 OH                                                                     (+)-pin                                       917                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 Me                                                                    (+)-pin CP                                    918                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                       919                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                       920                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             Ph       (+)-pin AQ                                    921                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             PhCH.sub.2                                                                              (+)-pin AR                                    922                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             Ph(CH.sub.2).sub.2                                                                      (+)-pin                                       923                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-NO.sub.2 -Ph                                                                          (+)-pin AS                                    924                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             4-NO.sub.2 -Ph                                                                          (+)-pin                                       925                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CO.sub.2 H-Ph                                                                         (+)-pin                                       926                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             4-CO.sub.2 H-Ph                                                                         (+)-pin                                       927                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CN.sub.4 H-Ph                                                                         (+)-pin                                       928                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             4-CN.sub.4 H-Ph                                                                         (+)-pin                                       929                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                       930                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                       931                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-NH.sub.2 -Ph                                                                          (+)-pin CQ                                    932                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             H        (+)-pin                                       933                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             Methyl   (+)-pin                                       934                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             Ethyl    (+)-pin                                       935                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             n-Propyl (+)-pin                                       936                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             n-Butyl  (+)-pin                                       937                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 SCH.sub.3                                                                      (+)-pin                                       938                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                       939                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                       940                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                       941                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                       942                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                       943                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                       944                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                       945                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                       946                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CF.sub.3 (+)-pin                                       947                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.3                                                                       (+)-pin                                       948                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                       949                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                       950                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             F.sub.5 -Ph                                                                             (+)-pin                                       951                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                       952                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                       953                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                       954                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                       955                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                       956                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2)CH.sub.3 CN.sub.4 H                                                           (+)-pin                                       957                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                       958                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                       959                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                       960                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 OH                                                                             (+)-pin                                       961                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                       962                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 OH                                                                     (+)-pin                                       963                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                       964                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                       965                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                       966                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             Ph       (+)-pin                                       967                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             PhCH.sub.2                                                                              (+)-pin AT                                    968                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             Ph(CH.sub.2).sub.2                                                                      (+)-pin                                       969                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             3-NO.sub.2 -Ph                                                                          (+)-pin AU                                    970                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             4-NO.sub.2 Ph                                                                           (+)-pin                                       971                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             3-CO.sub.2 H-Ph                                                                         (+)-pin                                       972                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             4-CO.sub.2 H-Ph                                                                         (+)-pin                                       973                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             3-CN.sub.4 H-Ph                                                                         (+)-pin                                       974                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             4-CN.sub.4 H-Ph                                                                         (+)-pin                                       975                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                       976                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                       977                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             H        OH, OH  AI                                    978                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             Methyl   OH, OH                                        979                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             Ethyl    OH, OH                                        980                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             n-Propyl OH, OH                                        981                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             n-Butyl  OH, OH                                        982                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 SCH.sub.3                                                                      OH, OH                                        983                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                        984                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                        985                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                        986                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                        987                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                        988                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                        989                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                        990                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                        991                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CF.sub.3 OH, OH                                        992                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.3                                                                       OH, OH                                        993                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                        994                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                        995                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             F.sub.5 -Ph                                                                             OH, OH                                        996                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 H                                                                     OH, OH                                        997                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                        998                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                        999                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CN.sub.4 H                                                                     OH, OH                                       1000                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                       1001                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                       1002                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       1003                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                       1004                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                       1005                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 OH                                                                             OH, OH                                       1006                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       1007                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 OH                                                                     OH, OH                                       1008                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                       1009                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                       1010                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                       1011                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             Ph       OH, OH  AV                                   1012                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             PhCH.sub.2                                                                              OH, OH                                       1013                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             Ph(CH.sub.2).sub.2                                                                      OH, OH                                       1014                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-NO.sub.2 -Ph                                                                          OH, OH                                       1015                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             4-NO.sub.2 -Ph                                                                          OH, OH                                       1016                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CO.sub.2 H-Ph                                                                         OH, OH                                       1017                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             4-CO.sub.2 H-Ph                                                                         OH, OH                                       1018                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CN.sub.4 H-Ph                                                                         OH, OH                                       1019                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             4-CN.sub.4 H-Ph                                                                         OH, OH                                       1020                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1021                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             4-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1022                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             F        (+)-pin                                      1023                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             Cl       (+)-pin                                      1024                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             Br       (+)-pin                                      1025                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             I        (+)-pin                                      1026                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             COOH     (+)-pin                                      1027                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             COOMe    (+)-pin                                      1028                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CHO      (+)-pin                                      1029                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             COMe     (+)-pin                                      1030                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             NO.sub.2 (+)-pin                                      1031                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CN       (+)-pin                                      1032                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             isopropyl                                                                               (+)-pin                                      1033                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-F-phenyl                                                                              (+)-pin                                      1034                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-Cl-phenyl                                                                             (+)-pin                                      1035                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             4-Br-phenyl                                                                             (+)-pin                                      1036                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             4-I-phenyl                                                                              (+)-pin                                      1037                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CH.sub.3 -phenyl                                                                      (+)-pin                                      1038                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-MeO-phenyl                                                                            (+)-pin                                      1039                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CN-phenyl                                                                             (+)-pin                                      1040                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             4-CN-phenyl                                                                             (+)-pin                                      1041                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-NC-phenyl                                                                             (+)-pin                                      1042                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             4-NC-phenyl                                                                             (+)-pin                                      1043                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CF.sub.3 -phenyl                                                                      (+)-pin                                      1044                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CH.sub.2 S-phenyl                                                                     (+)-pin                                      1045                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CH.sub.3 SO-phenyl                                                                    (+)-pin                                      1046                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CH.sub.3 SO.sub.2 -phenyl                                                             (+)-pin                                      1047                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-N(Me).sub.2 -phenyl                                                                   (+)-pin                                      1048                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-MeCO-phenyl                                                                           (+)-pin                                      1049                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CHO-phenyl                                                                            (+)-pin                                      1050                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CO.sub.2 Me-phenyl                                                                    (+)-pin                                      1051                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CONH.sub.2 -phenyl                                                                    (+)-pin                                      1052                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 NHSO.sub.2 CF.sub.3                                                            (+)-pin                                      1053                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 NHSO.sub.2 CH.sub.3                                                            (+)-pin                                      1054                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 -i-propyl                                                             (+)-pin                                      1055                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CHO                                                                            (+)-pin                                      1056                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 OMe                                                                   (+)-pin                                      1057                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 O-i-propyl                                                            (+)-pin                                      1058                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 OCOMe                                                                          (+)-pin                                      1059                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 OCO-i-propyl                                                                   (+)-pin                                      1060                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 OCO-Phenyl                                                                     (+)-pin                                      1061                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 NHCOMe                                                                         (+)-pin                                      1062                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 NHCO-i-propyl                                                                  (+)-pin                                      1063                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             F        OH, OH                                       1064                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             Cl       OH, OH                                       1065                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             Br       OH, OH                                       1066                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             I        OH, OH                                       1067                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             COOH     OH, OH                                       1068                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             COOMe    OH, OH                                       1069                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CHO      OH, OH                                       1070                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             COMe     OH, OH                                       1071                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             NO.sub.2 OH, OH                                       1072                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CN       OH, OH                                       1073                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             isopropyl                                                                               OH, OH                                       1074                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-F-phenyl                                                                              OH, OH                                       1075                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-Cl-phenyl                                                                             OH, OH                                       1076                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             4-Br-phenyl                                                                             OH, OH                                       1077                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             4-I-phenyl                                                                              OH, OH                                       1078                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CH.sub.3 -phenyl                                                                      OH, OH                                       1079                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-MeO-phenyl                                                                            OH, OH                                       1080                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CN-phenyl                                                                             OH, OH                                       1081                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             4-CN-phenyl                                                                             OH, OH                                       1082                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-NC-phenyl                                                                             OH, OH                                       1083                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             4-NC-phenyl                                                                             OH, OH                                       1084                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CF.sub.3 -phenyl                                                                      OH, OH                                       1085                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CH.sub.2 S-phenyl                                                                     OH, OH                                       1086                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CH.sub.3 SO-phenyl                                                                    OH, OH                                       1087                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CH.sub.3 SO.sub.2 -phenyl                                                             OH, OH                                       1088                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-N(Me).sub.2 -phenyl                                                                   OH, OH                                       1089                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-MeCO-phenyl                                                                           OH, OH                                       1090                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CHO-phenyl                                                                            OH, OH                                       1091                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CO.sub.2 Me-phenyl                                                                    OH, OH                                       1092                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-CONH.sub.2 -phenyl                                                                    OH, OH                                       1093                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 NHSO.sub.2 CF.sub.3                                                            OH, OH                                       1094                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 NHSO.sub.2 CH.sub.3                                                            OH, OH                                       1095                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 -i-propyl                                                             OH, OH                                       1096                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CHO                                                                            OH, OH                                       1097                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 OMe                                                                   OH, OH                                       1098                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 O-i-propyl                                                            OH, OH                                       1099                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 OCOMe                                                                          OH, OH                                       1100                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 OCO-i-propyl                                                                   OH, OH                                       1101                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 OCO-Phenyl                                                                     OH, OH                                       1102                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 NHCOMe                                                                         OH, OH                                       1103                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 NHCO-i-propyl                                                                  OH, OH                                       1104                                                                              CH.sub.2 NH.sub.2                                                                          1 3,4-Di-F-PhCH.sub.2                                                                    CH.sub.2 CN                                                                             (+)-pin                                      1105                                                                              CH.sub.2 NH.sub.2                                                                          1 3,4-Di-Cl-PhCH.sub.2                                                                   CH.sub.2 CN                                                                             (+)-pin                                      1106                                                                              CH.sub.2 NH.sub.2                                                                          1 4-Br-PhCH.sub.2                                                                        CH.sub.2 CN                                                                             (+)-pin                                      1107                                                                              CH.sub.2 NH.sub.2                                                                          1 4-I-PhCH.sub.2                                                                         CH.sub.2 CN                                                                             (+)-pin                                      1108                                                                              CH.sub.2 NH.sub.2                                                                          1 4-Me-PhCH.sub.2                                                                        CH.sub.2 CN                                                                             (+)-pin                                      1109                                                                              CH.sub.2 NH.sub.2                                                                          1 2-MeO-PhCH.sub.2                                                                       CH.sub.2 CN                                                                             (+)-pin                                      1110                                                                              CH.sub.2 NH.sub.2                                                                          1 2-CN-PhCH.sub.2                                                                        CH.sub.2 CN                                                                             (+)-pin                                      1111                                                                              CH.sub.2 NH.sub.2                                                                          1 2-NC-PhCH.sub.2                                                                        CH.sub.2 CN                                                                             (+)-pin                                      1112                                                                              CH.sub.2 NH.sub.2                                                                          1 2-NO.sub.2 -PhCH.sub.2                                                                 CH.sub.2 CN                                                                             (+)-pin                                      1113                                                                              CH.sub.2 NH.sub.2                                                                          1 2-CF.sub.3 -PhCH.sub.2                                                                 CH.sub.2 CN                                                                             (+)-pin                                      1114                                                                              CH.sub.2 NH.sub.2                                                                          1 2-MeS-PhCH.sub.2                                                                       CH.sub.2 CN                                                                             (+)-pin                                      1115                                                                              CH.sub.2 NH.sub.2                                                                          1 3-MeSO-PhCH.sub.2                                                                      CH.sub.2 CN                                                                             (+)-pin                                      1116                                                                              CH.sub.2 NH.sub.2                                                                          1 3-MeSO.sub.2 -PhCH.sub.2                                                               CH.sub.2 CN                                                                             (+)-pin                                      1117                                                                              CH.sub.2 NH.sub.2                                                                          1 2-NH.sub.2 -PhCH.sub.2                                                                 CH.sub.2 CN                                                                             (+)-pin                                      1118                                                                              CH.sub.2 NH.sub.2                                                                          1 3-NHMe-PhCH.sub.2                                                                      CH.sub.2 CN                                                                             (+)-pin                                      1119                                                                              CH.sub.2 NH.sub.2                                                                          1 2-CHO-PhCH.sub.2                                                                       CH.sub.2 CN                                                                             (+)-pin                                      1120                                                                              CH.sub.2 NH.sub.2                                                                          1 3-MeCO-PhCH.sub.2                                                                      CH.sub.2 CN                                                                             (+)-pin                                      1121                                                                              CH.sub.2 NH.sub.2                                                                          1 2-MeO.sub.2 C-PhCH.sub.2                                                               CH.sub.2 CN                                                                             (+)-pin                                      1122                                                                              CH.sub.2 NH.sub.2                                                                          1 2-NH.sub.2 OC-PhCH.sub.2                                                               CH.sub.2 CN                                                                             (+)-pin                                      1123                                                                              CH.sub.2 NH.sub.2                                                                          1 2-HOCH.sub.2 -PhCH.sub.2                                                               CH.sub.2 CN                                                                             (+)-pin                                      1124                                                                              CH.sub.2 NH.sub.2                                                                          1 3,4-Di-F-PhCH.sub.2                                                                    CH.sub.2 CN                                                                             OH, OH                                       1125                                                                              CH.sub.2 NH.sub.2                                                                          1 3,4-Di-Cl-PhCH.sub.2                                                                   CH.sub.2 CN                                                                             OH, OH                                       1126                                                                              CH.sub.2 NH.sub.2                                                                          1 4-Br-PhCH.sub.2                                                                        CH.sub.2 CN                                                                             OH, OH                                       1127                                                                              CH.sub.2 NH.sub.2                                                                          1 4-I-PhCH.sub.2                                                                         CH.sub.2 CN                                                                             OH, OH                                       1128                                                                              CH.sub.2 NH.sub.2                                                                          1 4-Me-PhCH.sub.2                                                                        CH.sub.2 CN                                                                             OH, OH                                       1129                                                                              CH.sub.2 NH.sub.2                                                                          1 2-MeO-PhCH.sub.2                                                                       CH.sub.2 CN                                                                             OH, OH                                       1130                                                                              CH.sub.2 NH.sub.2                                                                          1 2-CN-PhCH.sub.2                                                                        CH.sub.2 CN                                                                             OH, OH                                       1131                                                                              CH.sub.2 NH.sub.2                                                                          1 2-NC-PhCH.sub.2                                                                        CH.sub.2 CN                                                                             OH, OH                                       1132                                                                              CH.sub.2 NH.sub.2                                                                          1 2-NO.sub.2 -PhCH.sub.2                                                                 CH.sub.2 CN                                                                             OH, OH                                       1133                                                                              CH.sub.2 NH.sub.2                                                                          1 2-CF.sub.3 -PhCH.sub.2                                                                 CH.sub.2 CN                                                                             OH, OH                                       1134                                                                              CH.sub.2 NH.sub.2                                                                          1 2-MeS-PhCH.sub.2                                                                       CH.sub.2 CN                                                                             OH, OH                                       1135                                                                              CH.sub.2 NH.sub.2                                                                          1 3-MeSO-PhCH.sub.2                                                                      CH.sub.2 CN                                                                             OH, OH                                       1136                                                                              CH.sub.2 NH.sub.2                                                                          1 3-MeSO.sub.2 -PhCH.sub.2                                                               CH.sub.2 CN                                                                             OH, OH                                       1137                                                                              CH.sub.2 NH.sub.2                                                                          1 2-NH.sub.2 -PhCH.sub.2                                                                 CH.sub.2 CN                                                                             OH, OH                                       1138                                                                              CH.sub.2 NH.sub.2                                                                          1 3-NHMe-PhCH.sub.2                                                                      CH.sub.2 CN                                                                             OH, OH                                       1139                                                                              CH.sub.2 NH.sub.2                                                                          1 2-CHO-PhCH.sub.2                                                                       CH.sub.2 CN                                                                             OH, OH                                       1140                                                                              CH.sub.2 NH.sub.2                                                                          1 3-MeCO-PhCH.sub.2                                                                      CH.sub.2 CN                                                                             OH, OH                                       1141                                                                              CH.sub.2 NH.sub.2                                                                          1 2-MeO.sub.2 C-PhCH.sub.2                                                               CH.sub.2 CN                                                                             OH, OH                                       1142                                                                              CH.sub.2 NH.sub.2                                                                          1 2-NH.sub.2 OC-PhCH.sub.2                                                               CH.sub.2 CN                                                                             OH, OH                                       1143                                                                              CH.sub.2 NH.sub.2                                                                          1 2-HOCH.sub.2 -PhCH.sub.2                                                               CH.sub.2 CN                                                                             OH, OH                                       1144                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             H        OH, OH                                       1145                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             Methyl   OH, OH                                       1146                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             Ethyl    OH, OH                                       1147                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             n-Propyl OH, OH                                       1148                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             n-Butyl  OH, OH                                       1149                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 SCH.sub.3                                                                      OH, OH                                       1150                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                       1151                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                       1152                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                       1153                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                       1154                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                       1155                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1156                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                       1157                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                       1158                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CF.sub.3 OH, OH                                       1159                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.3                                                                       OH, OH                                       1160                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                       1161                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                       1162                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             F.sub.5 -Ph                                                                             OH, OH                                       1163                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 H                                                                     OH, OH                                       1164                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                       1165                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                       1166                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CN.sub.4 H                                                                     OH, OH                                       1167                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                       1168                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                       1169                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       1170                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                       1171                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                       1172                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 OH                                                                             OH, OH                                       1173                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       1174                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 OH                                                                     OH, OH                                       1175                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                       1176                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                       1177                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                       1178                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             Ph       OH, OH                                       1179                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             PhCH.sub.2                                                                              OH, OH                                       1180                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             Ph(CH.sub.2).sub.2                                                                      OH, OH                                       1181                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             3-NO.sub.2 -Ph                                                                          OH, OH                                       1182                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             4-NO.sub.2 -Ph                                                                          OH, OH                                       1183                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             3-CO.sub.2 H-Ph                                                                         OH, OH                                       1184                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             4-CO.sub.2 H-Ph                                                                         OH, OH                                       1185                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             3-CN.sub.4 H-Ph                                                                         OH, OH                                       1186                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             4-CN.sub.4 H-Ph                                                                         OH, OH                                       1187                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             3-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1188                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             4-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1189                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CHO                                                                            (+)-pin                                      1190                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CHO                                                                            OH, OH                                       1191                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CHO                                                                            (+)-pin                                      1192                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CHO                                                                            OH, OH                                       1193                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             H        (+)-pin                                      1194                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             Methyl   (+)-pin                                      1195                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             Ethyl    (+)-pin                                      1196                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             n-Propyl (+)-pin                                      1197                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             n-Butyl  (+)-pin                                      1198                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 SCH.sub.3                                                                      (+)-pin                                      1199                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                      1200                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                      1201                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                      1202                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                      1203                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                      1204                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1205                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                      1206                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                      1207                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CF.sub.3 (+)-pin                                      1208                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.3                                                                       (+)-pin                                      1209                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                      1210                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                      1211                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             F.sub.5 -Ph                                                                             (+)-pin                                      1212                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                      1213                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                      1214                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                      1215                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                      1216                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                      1217                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                      1218                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      1219                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                      1220                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                      1221                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 OH                                                                             (+)-pin                                      1222                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      1223                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 OH                                                                     (+)-pin                                      1224                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                      1225                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                      1226                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                      1227                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             Ph       (+)-pin                                      1228                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             PhCH.sub.2                                                                              (+)-pin                                      1229                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             Ph(CH.sub.2).sub.2                                                                      (+)-pin                                      1230                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             3-NO.sub.2 -Ph                                                                          (+)-pin                                      1231                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             4-NO.sub.2 -Ph                                                                          (+)-pin                                      1232                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             3-CO.sub.2 H-Ph                                                                         (+)-pin                                      1233                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             4-CO.sub.2 H-Ph                                                                         (+)-pin                                      1234                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             3-CN.sub.4 H-Ph                                                                         (+)-pin                                      1235                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             4-CN.sub.4 H-Ph                                                                         (+)-pin                                      1236                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      1237                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      1238                                                                              CN          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1239                                                                              NO.sub.2    1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1240                                                                              CH.sub.2 NO.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1241                                                                              CF.sub.3    1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1242                                                                              NH.sub.2    1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1243                                                                              NHOH        1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1244                                                                              NHOME       1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1245                                                                              CH.sub.2 NHOH                                                                              1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1246                                                                              CH.sub.2 NHOMe                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1247                                                                              NH(CNH)CH.sub.3                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1248                                                                              NH(CNH)NHOH 1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1249                                                                              NH(CNH)NHNH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1250                                                                              NH(CNH)NHCN 1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1251                                                                              NH(CNH)NHCH.sub.3                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1252                                                                              NH(CNH)NHCOCH.sub.3                                                                        1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1253                                                                              C(NH)NH.sub.2                                                                              1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1254                                                                              C(NH)NHMe   1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1255                                                                              C(NH)NHCOMe 1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1256                                                                              CONH.sub.2  1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1257                                                                              CONHCH.sub.3                                                                               1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1258                                                                              CO.sub.2 CH.sub.3                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1259                                                                              OH          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1260                                                                              CH.sub.2 OH 1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1261                                                                              SCH.sub.3   1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1262                                                                              SOCH.sub.3  1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1263                                                                              SO.sub.2 CH.sub.3                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1264                                                                              S(CNH)NHCH.sub.3                                                                           1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1265                                                                              S(CNH)NHCOCH.sub.3                                                                         1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1266                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             H        OH, OH                                       1267                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             Methyl   OH, OH                                       1268                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             Ethyl    OH, OH                                       1269                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             n-Propyl OH, OH                                       1270                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             n-Butyl  OH, OH                                       1271                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 SCH.sub.3                                                                      OH, OH                                       1272                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                       1273                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                       1274                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                       1275                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                       1276                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                       1277                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1278                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                       1279                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                       1280                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CF.sub.3 OH, OH                                       1281                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.3                                                                       OH, OH                                       1282                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                       1283                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                       1284                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             F.sub.5 -Ph                                                                             OH, OH                                       1285                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 H                                                                     OH, OH                                       1286                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                       1287                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                       1288                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CN.sub.4 H                                                                     OH, OH                                       1289                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                       1290                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                       1291                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       1292                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                       1293                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                       1294                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 OH                                                                             OH, OH                                       1295                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       1296                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 OH                                                                     OH, OH                                       1297                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                       1298                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                       1299                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                       1300                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             Ph       OH, OH                                       1301                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             PhCH.sub.2                                                                              OH, OH                                       1302                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             Ph(CH.sub.2).sub.2                                                                      OH, OH                                       1303                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             3-NO.sub.2 -Ph                                                                          OH, OH                                       1304                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             4-NO.sub.2 -Ph                                                                          OH, OH                                       1305                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             3-CO.sub.2 H-Ph                                                                         OH, OH                                       1306                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             4-CO.sub.2 H-Ph                                                                         OH, OH                                       1307                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             3-CN.sub.4 H-Ph                                                                         OH, OH                                       1308                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             4-CN.sub.4 H-Ph                                                                         OH, OH                                       1309                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             3-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1310                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2                                                                             4-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1311                                                                              CN          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1312                                                                              NO.sub.2    1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1313                                                                              CH.sub.2 NO.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1314                                                                              CF.sub.3    1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1315                                                                              NH.sub.2    1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1316                                                                              NHOH        1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1317                                                                              NHOME       1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1318                                                                              CH.sub.2 NHOH                                                                              1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1319                                                                              CH.sub.2 NHOMe                                                                             1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1320                                                                              NH(CNH)CH.sub.3                                                                            1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1321                                                                              NH(CNH)NHOH 1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1322                                                                              NH(CNH)NHNH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1323                                                                              NH(CNH)NHCN 1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1324                                                                              NH(CNH)NHCH.sub.3                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1325                                                                              NH(CNH)NHCOCH.sub.3                                                                        1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1326                                                                              C(NH)NH.sub.2                                                                              1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1327                                                                              C(NH)NHMe   1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1328                                                                              C(NH)NHCOMe 1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1329                                                                              CONH.sub.2  1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1330                                                                              CONHCH.sub.3                                                                               1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1331                                                                              CO.sub.2 CH.sub.3                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1332                                                                              OH          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1333                                                                              CH.sub.2 OH 1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1334                                                                              SCH.sub.3   1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1335                                                                              SOCH.sub.3  1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1336                                                                              SO.sub.2 CH.sub.3                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1337                                                                              S(CNH)NHCH.sub.3                                                                           1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1338                                                                              S(CNH)NHCOCH.sub.3                                                                         1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1339                                                                              CH.sub.2 NH.sub.2                                                                          2 PhCH.sub.2                                                                             H        (+)-pin                                      1340                                                                              CH.sub.2 NH.sub.2                                                                          2 PhCH.sub.2                                                                             H        OH, OH                                       1341                                                                              OMe         1 PhCH.sub.2                                                                             H        (+)-pin                                      1342                                                                              OMe         1 PhCH.sub.2                                                                             Methyl   (+)-pin                                      1343                                                                              OMe         1 PhCH.sub.2                                                                             Ethyl    (+)-pin                                      1344                                                                              OMe         1 PhCH.sub.2                                                                             n-Propyl (+)-pin                                      1345                                                                              OMe         1 PhCH.sub.2                                                                             n-Butyl  (+)-pin                                      1346                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 SCH.sub.3                                                                      (+)-pin                                      1347                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                      1348                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                      1349                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                      1350                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                      1351                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                      1352                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin CR                                   1353                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                      1354                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                      1355                                                                              OMe         1 PhCH.sub.2                                                                             CF.sub.3 (+)-pin                                      1356                                                                              OMe         1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.3                                                                       (+)-pin                                      1357                                                                              OMe         1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                      1358                                                                              OMe         1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                      1359                                                                              OMe         1 PhCH.sub.2                                                                             F.sub.5 -Ph                                                                             (+)-pin                                      1360                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                      1361                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                      1362                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                      1363                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                      1364                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                      1365                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                      1366                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      1367                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                      1368                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                      1369                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 OH                                                                             (+)-pin                                      1370                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      1371                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 OH                                                                     (+)-pin                                      1372                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                      1373                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                      1374                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                      1375                                                                              OMe         1 PhCH.sub.2                                                                             Ph       (+)-pin                                      1376                                                                              OMe         1 PhCH.sub.2                                                                             PhCH.sub.2                                                                              (+)-pin                                      1377                                                                              OMe         1 PhCH.sub.2                                                                             Ph(CH.sub.2).sub.2                                                                      (+)-pin                                      1378                                                                              OMe         1 PhCH.sub.2                                                                             3-NO.sub.2 -Ph                                                                          (+)-pin                                      1379                                                                              OMe         1 PhCH.sub.2                                                                             4-NO.sub.2 -Ph                                                                          (+)-pin                                      1380                                                                              OMe         1 PhCH.sub.2                                                                             3-CO.sub.2 H-Ph                                                                         (+)-pin                                      1381                                                                              OMe         1 PhCH.sub.2                                                                             4-CO.sub.2 H-Ph                                                                         (+)-pin                                      1382                                                                              OMe         1 PhCH.sub.2                                                                             3-CN.sub.4 H-Ph                                                                         (+)-pin                                      1383                                                                              OMe         1 PhCH.sub.2                                                                             4-CN.sub.4 H-Ph                                                                         (+)-pin                                      1384                                                                              OMe         1 PhCH.sub.2                                                                             3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      1385                                                                              OMe         1 PhCH.sub.2                                                                             4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      1386                                                                              OMe         1 PhCH.sub.2                                                                             H        OH, OH                                       1387                                                                              OMe         1 PhCH.sub.2                                                                             Methyl   OH, OH                                       1388                                                                              OMe         1 PhCH.sub.2                                                                             Ethyl    OH, OH                                       1389                                                                              OMe         1 PhCH.sub.2                                                                             n-Propyl OH, OH                                       1390                                                                              OMe         1 PhCH.sub.2                                                                             n-Butyl  OH, OH                                       1391                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 SCH.sub.3                                                                      OH, OH                                       1392                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                       1393                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                       1394                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                       1395                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                       1396                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                       1397                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1398                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                       1399                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                       1400                                                                              OMe         1 PhCH.sub.2                                                                             CF.sub.3 OH, OH                                       1401                                                                              OMe         1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.3                                                                       OH, OH                                       1402                                                                              OMe         1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                       1403                                                                              OMe         1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                       1404                                                                              OMe         1 PhCH.sub.2                                                                             F.sub.5 -Ph                                                                             OH, OH                                       1405                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 H                                                                     OH, OH                                       1406                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                       1407                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                       1408                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CN.sub.4 H                                                                     OH, OH                                       1409                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                       1410                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                       1411                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       1412                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                       1413                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                       1414                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 OH                                                                             OH, OH                                       1415                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       1416                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 OH                                                                     OH, OH                                       1417                                                                              OMe         1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                       1418                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                       1419                                                                              OMe         1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                       1420                                                                              OMe         1 PhCH.sub.2                                                                             PhCH.sub.2                                                                              OH, OH                                       1421                                                                              OMe         1 PhCH.sub.2                                                                             PhCH.sub.2                                                                              OH, OH                                       1422                                                                              OMe         1 PhCH.sub.2                                                                             Ph(CH.sub.2).sub.2                                                                      OH, OH                                       1423                                                                              OMe         1 PhCH.sub.2                                                                             3-NO.sub.2 -Ph                                                                          OH, OH                                       1424                                                                              OMe         1 PhCH.sub.2                                                                             4-NO.sub.2 -Ph                                                                          OH, OH                                       1425                                                                              OMe         1 PhCH.sub.2                                                                             3-CO.sub.2 H-Ph                                                                         OH, OH                                       1426                                                                              OMe         1 PhCH.sub.2                                                                             4-CO.sub.2 H-Ph                                                                         OH, OH                                       1427                                                                              OMe         1 PhCH.sub.2                                                                             3-CN.sub.4 H-Ph                                                                         OH, OH                                       1428                                                                              OMe         1 PhCH.sub.2                                                                             4-CN.sub.4 H-Ph                                                                         OH, OH                                       1429                                                                              OMe         1 PhCH.sub.2                                                                             3-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1430                                                                              OMe         1 PhCH.sub.2                                                                             4-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1431                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    H        (+)-pin AX                                   1432                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    Methyl   (+)-pin                                      1433                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    Ethyl    (+)-pin                                      1434                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    n-Propyl (+)-pin                                      1435                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    n-Butyl  (+)-pin                                      1436                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 SCH.sub.3                                                                      (+)-pin                                      1437                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                      1438                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                      1439                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                      1440                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                      1441                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                      1442                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN                                                                             (+)-pin                                      1443                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                      1444                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                      1445                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.3 (+)-pin                                      1446                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.3                                                                       (+)-pin                                      1447                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                      1448                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                      1449                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    F.sub.5 -Ph                                                                             (+)-pin                                      1450                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                      1451                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                      1452                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                      1453                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                      1454                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                      1455                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                      1456                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 NO.sub.2                                                                       (+)-pin                                      1457                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                      1458                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                      1459                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 OH                                                                             (+)-pin CS                                   1460                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      1461                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 OH                                                                     (+)-pin                                      1462                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                      1463                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                      1464                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                      1465                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    Ph       (+)-pin                                      1466                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    PhCH.sub.2                                                                              (+)-pin                                      1467                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    Ph(CH.sub.2).sub.2                                                                      (+)-pin AY                                   1468                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    3-NO.sub.2 -Ph                                                                          (+)-pin                                      1469                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    4-NO.sub.2 -Ph                                                                          (+)-pin                                      1470                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    3-CO.sub.2 H-Ph                                                                         (+)-pin                                      1471                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    4-CO.sub.2 H-Ph                                                                         (+)-pin                                      1472                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    3-CN.sub.4 H-Ph                                                                         (+)-pin                                      1473                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    4-CN.sub.4 H-Ph                                                                         (+)-pin                                      1474                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      1475                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      1476                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    H        (+)-pin                                      1477                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    Methyl   (+)-pin                                      1478                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    Ethyl    (+)-pin                                      1479                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    n-Propyl (+)-pin                                      1480                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    n-Butyl  (+)-pin                                      1481                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 SCH.sub.3                                                                      (+)-pin                                      1482                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                      1483                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                      1484                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                      1485                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                      1486                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                      1487                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN                                                                             (+)-pin                                      1488                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                      1489                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                      1490                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.3 (+)-pin                                      1491                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.3                                                                       (+)-pin                                      1492                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                      1493                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                      1494                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    F.sub.5 -Ph                                                                             (+)-pin                                      1495                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                      1496                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                      1497                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                      1498                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                      1499                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                      1500                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                      1501                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 NO.sub.2                                                                       (+)-pin                                      1502                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                      1503                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                      1504                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 OH                                                                             (+)-pin                                      1505                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      1506                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 OH                                                                     (+)-pin                                      1507                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                      1508                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                      1509                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                      1510                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    Ph       (+)-pin                                      1511                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    PhCH.sub.2                                                                              (+)-pin                                      1512                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    Ph(CH.sub.2).sub.2                                                                      (+)-pin                                      1513                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    3-NO.sub.2 -Ph                                                                          (+)-pin                                      1514                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    4-NO.sub.2 -Ph                                                                          (+)-pin                                      1515                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    3-CO.sub.2 H-Ph                                                                         (+)-pin                                      1516                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    4-CO.sub.2 H-Ph                                                                         (+)-pin                                      1517                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    3-CN.sub.4 H-Ph                                                                         (+)-pin                                      1518                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    4-CN.sub.4 H-Ph                                                                         (+)-pin                                      1519                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      1520                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      1521                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    H        OH, OH  AZ                                   1522                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    Methyl   OH, OH                                       1523                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    Ethyl    OH, OH                                       1524                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    n-Propyl OH, OH                                       1525                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    n-Butyl  OH, OH                                       1526                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 SCH.sub.3                                                                      OH, OH                                       1527                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                       1528                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                       1529                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                       1530                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                       1531                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                       1532                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN                                                                             OH, OH                                       1533                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                       1534                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                       1535                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.3 OH, OH                                       1536                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.3                                                                       OH, OH                                       1537                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                       1538                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                       1539                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    F.sub.5 -Ph                                                                             OH, OH                                       1540                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 H                                                                     OH, OH                                       1541                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                       1542                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                       1543                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN.sub.4 H                                                                     OH, OH                                       1544                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                       1545                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                       1546                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 NO.sub.2                                                                       OH, OH                                       1547                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                       1548                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                       1549                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 OH                                                                             OH, OH                                       1550                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 OH                                                                     OH, OH                                       1551                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 OH                                                                     OH, OH                                       1552                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                       1553                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                       1554                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                       1555                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    Ph       OH, OH                                       1556                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    PhCH.sub.2                                                                              OH, OH                                       1557                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    Ph(CH.sub.2).sub.2                                                                      OH, OH  AJ                                   1558                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    3-NO.sub.2 -Ph                                                                          OH, OH                                       1559                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    4-NO.sub.2 -Ph                                                                          OH, OH                                       1560                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    3-CO.sub.2 H-Ph                                                                         OH, OH                                       1561                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    4-CO.sub.2 H-Ph                                                                         OH, OH                                       1562                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    3-CN.sub.4 H-Ph                                                                         OH, OH                                       1563                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    4-CN.sub.4 H-Ph                                                                         OH, OH                                       1564                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    3-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1565                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    4-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1566                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    H        OH, OH                                       1567                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    Methyl   OH, OH                                       1568                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    Ethyl    OH, OH                                       1569                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    n-Propyl OH, OH                                       1570                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    n-Butyl  OH, OH                                       1571                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 SCH.sub.3                                                                      OH, OH                                       1572                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                       1573                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                       1574                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                       1575                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                       1576                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                       1577                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN                                                                             OH, OH                                       1578                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                       1579                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                       1580                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.3 OH, OH                                       1581                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.3                                                                       OH, OH                                       1582                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                       1583                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                       1584                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    F.sub.5 -Ph                                                                             OH, OH                                       1585                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 H                                                                     OH, OH                                       1586                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                       1587                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                       1588                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN.sub.4 H                                                                     OH, OH                                       1589                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                       1590                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                       1591                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 NO.sub.2                                                                       OH, OH                                       1592                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                       1593                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                       1594                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 OH                                                                             OH, OH                                       1595                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 OH                                                                     OH, OH                                       1596                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 OH                                                                     OH, OH                                       1597                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                       1598                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                       1599                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                       1600                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    PhCH.sub.2 CH.sub.2                                                                     OH, OH                                       1601                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    PhCH.sub.2 CH.sub.2                                                                     OH, OH                                       1602                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    Ph(CH.sub.2).sub.2                                                                      OH, OH                                       1603                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    3-NO.sub.2 -Ph                                                                          OH, OH                                       1604                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    4-NO.sub.2 -Ph                                                                          OH, OH                                       1605                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    3-CO.sub.2 H-Ph                                                                         OH, OH                                       1606                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    4-CO.sub.2 H-Ph                                                                         OH, OH                                       1607                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    3-CN.sub.4 H-Ph                                                                         OH, OH                                       1608                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    4-CN.sub.4 H-Ph                                                                         OH, OH                                       1609                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    3-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1610                                                                              NH(CNH)NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                    4-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1611                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    H        (+)-pin                                      1612                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    Methyl   (+)-pin                                      1613                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    Ethyl    (+)-pin                                      1614                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    n-Propyl (+)-pin                                      1615                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    n-Butyl  (+)-pin                                      1616                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 SCH.sub.3                                                                      (+)-pin                                      1617                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                      1618                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                      1619                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                      1620                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                      1621                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                      1622                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN                                                                             (+)-pin                                      1623                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                      1624                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                      1625                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.3 (+)-pin                                      1626                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.3                                                                       (+)-pin                                      1627                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                      1628                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                      1629                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    F.sub.5 -Ph                                                                             (+)-pin                                      1630                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                      1631                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                      1632                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                      1633                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                      1634                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                      1635                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                      1636                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 NO.sub.2                                                                       (+)-pin                                      1637                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                      1638                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                      1639                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 OH                                                                             (+)-pin                                      1640                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      1641                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 OH                                                                     (+)-pin                                      1642                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                      1643                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                      1644                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                      1645                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    Ph       (+)-pin                                      1646                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    PhCH.sub.2                                                                              (+)-pin                                      1647                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    Ph(CH.sub.2).sub.2                                                                      (+)-pin                                      1648                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    3-NO.sub.2 -Ph                                                                          (+)-pin                                      1649                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    4-NO.sub.2 -Ph                                                                          (+)-pin                                      1650                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    3-CO.sub.2 H-Ph                                                                         (+)-pin                                      1651                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    4-CO.sub.2 H-Ph                                                                         (+)-pin                                      1652                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    3-CN.sub.4 H-Ph                                                                         (+)-pin                                      1653                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    4-CN.sub.4 H-Ph                                                                         (+)-pin                                      1654                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      1655                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      1656                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    H        OH, OH                                       1657                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    Methyl   OH, OH                                       1658                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    Ethyl    OH, OH                                       1659                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    n-Propyl OH, OH                                       1660                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    n-Butyl  OH, OH                                       1661                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 SCH.sub.3                                                                      OH, OH                                       1662                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                       1663                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                       1664                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                       1665                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                       1666                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                       1667                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN                                                                             OH, OH                                       1668                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                       1669                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                       1670                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.3 OH, OH                                       1671                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.3                                                                       OH, OH                                       1672                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                       1673                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                       1674                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    F.sub.5 -Ph                                                                             OH, OH                                       1675                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 H                                                                     OH, OH                                       1676                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                       1677                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                       1678                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN.sub.4 H                                                                     OH, OH                                       1679                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                       1680                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                       1681                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 NO.sub.2                                                                       OH, OH                                       1682                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                       1683                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                       1684                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 OH                                                                             OH, OH                                       1685                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 OH                                                                     OH, OH                                       1686                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 OH                                                                     OH, OH                                       1687                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                       1688                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                       1689                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                       1690                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    Ph       OH, OH                                       1691                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    PhCH.sub.2                                                                              OH, OH                                       1692                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    Ph(CH.sub.2).sub.2                                                                      OH, OH                                       1693                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    3-NO.sub.2 -Ph                                                                          OH, OH                                       1694                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    4-NO.sub.2 -Ph                                                                          OH, OH                                       1695                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    3-CO.sub.2 H-Ph                                                                         OH, OH                                       1696                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    4-CO.sub.2 H-Ph                                                                         OH, OH                                       1697                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    3-CN.sub.4 H-Ph                                                                         OH, OH                                       1698                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    4-CN.sub.4 H-Ph                                                                         OH, OH                                       1699                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    3-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1700                                                                              S(CNH)NH.sub.2                                                                             1 PhCH.sub.2 CH.sub.2                                                                    4-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1701                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    H        (+)-pin                                      1702                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    Methyl   (+)-pin                                      1703                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    Ethyl    (+)-pin                                      1704                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    n-Propyl (+)-pin                                      1705                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    n-Butyl  (+)-pin                                      1706                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 SCH.sub.3                                                                      (+)-pin                                      1707                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                      1708                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                      1709                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                      1710                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                      1711                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                      1712                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN                                                                             (+)-pin CR                                   1713                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                      1714                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                      1715                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.3 (+)-pin                                      1716                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.3                                                                       (+)-pin                                      1717                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                      1718                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                      1719                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    F.sub.5 -Ph                                                                             (+)-pin                                      1720                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                      1721                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                      1722                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                      1723                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                      1724                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                      1725                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                      1726                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 NO.sub.2                                                                       (+)-pin                                      1727                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                      1728                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                      1729                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 OH                                                                             (+)-pin                                      1730                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      1731                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 OH                                                                     (+)-pin                                      1732                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                      1733                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                      1734                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                      1735                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    Ph       (+)-pin                                      1736                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    PhCH.sub.2                                                                              (+)-pin                                      1737                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    Ph(CH.sub.2).sub.2                                                                      (+)-pin                                      1738                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    3-NO.sub.2 -Ph                                                                          (+)-pin                                      1739                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    4-NO.sub.2 -Ph                                                                          (+)-pin                                      1740                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    3-CO.sub.2 H-Ph                                                                         (+)-pin                                      1741                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    4-CO.sub.2 H-Ph                                                                         (+)-pin                                      1742                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    3-CN.sub.4 H-Ph                                                                         (+)-pin                                      1743                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    4-CN.sub.4 H-Ph                                                                         (+)-pin                                      1744                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      1745                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      1746                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    H        OH, OH                                       1747                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    Methyl   OH, OH                                       1748                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    Ethyl    OH, OH                                       1749                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    n-Propyl OH, OH                                       1750                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    n-Butyl  OH, OH                                       1751                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 SCH.sub.3                                                                      OH, OH                                       1752                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                       1753                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                       1754                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                       1755                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                       1756                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                       1757                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN                                                                             OH, OH                                       1758                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                       1759                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                       1760                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.3 OH, OH                                       1761                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.3                                                                       OH, OH                                       1762                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                       1763                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                       1764                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    F.sub.5 -Ph                                                                             OH, OH                                       1765                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 H                                                                     OH, OH                                       1766                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                       1767                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                       1768                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN.sub.4 H                                                                     OH, OH                                       1769                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                       1770                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                       1771                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 NO.sub.2                                                                       OH, OH                                       1772                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                       1773                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                       1774                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 OH                                                                             OH, OH                                       1775                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 OH                                                                     OH, OH                                       1776                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 OH                                                                     OH, OH                                       1777                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                       1778                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                       1779                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                       1780                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    Ph       OH, OH                                       1781                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    PhCH.sub.2                                                                              OH, OH                                       1782                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    Ph(CH.sub.2).sub.2                                                                      OH, OH                                       1783                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    3-NO.sub.2 -Ph                                                                          OH, OH                                       1784                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    4-NO.sub.2 -Ph                                                                          OH, OH                                       1785                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    3-CO.sub.2 H-Ph                                                                         OH, OH                                       1786                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    4-CO.sub.2 H-Ph                                                                         OH, OH                                       1787                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    3-CN.sub.4 H-Ph                                                                         OH, OH                                       1788                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    4-CN.sub.4 H-Ph                                                                         OH, OH                                       1789                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    3-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1790                                                                              OMe         1 PhCH.sub.2 CH.sub.2                                                                    4-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1791                                                                              NH(CNH)H    1 Ph      H        (+)-pin                                      1792                                                                              NH(CNH)H    1 Ph      Methyl   (+)-pin                                      1793                                                                              NH(CNH)H    1 Ph      Ethyl    (+)-pin                                      1794                                                                              NH(CNH)H    1 Ph      n-Propyl (+)-pin                                      1795                                                                              NH(CNH)H    1 Ph      n-Butyl  (+)-pin                                      1796                                                                              NH(CNH)H    1 Ph      CH.sub.2 SCH.sub.3                                                                      (+)-pin                                      1797                                                                              NH(CNH)H    1 Ph      CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                      1798                                                                              NH(CNH)H    1 Ph      CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                      1799                                                                              NH(CNH)H    1 Ph      CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                      1800                                                                              NH(CNH)H    1 Ph      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                      1801                                                                              NH(CNH)H    1 Ph      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                      1802                                                                              NH(CNH)H    1 Ph      CH.sub.2 CN                                                                             (+)-pin                                      1803                                                                              NH(CNH)H    1 Ph      CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                      1804                                                                              NH(CNH)H    1 Ph      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                      1805                                                                              NH(CNH)H    1 Ph      CF.sub.3 (+)-pin                                      1806                                                                              NH(CNH)H    1 Ph      CF.sub.2 CF.sub.3                                                                       (+)-pin                                      1807                                                                              NH(CNH)H    1 Ph      CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                      1808                                                                              NH(CNH)H    1 Ph      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                      1809                                                                              NH(CNH)H    1 Ph      F.sub.5 -Ph                                                                             (+)-pin                                      1810                                                                              NH(CNH)H    1 Ph      CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                      1811                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                      1812                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                      1813                                                                              NH(CNH)H    1 Ph      CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                      1814                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                      1815                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                      1816                                                                              NH(CNH)H    1 Ph      CH.sub.2 NO.sub.2                                                                       (+)-pin                                      1817                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                      1818                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                      1819                                                                              NH(CNH)H    1 Ph      CH.sub.2 OH                                                                             (+)-pin                                      1820                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      1821                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.3 OH                                                                     (+)-pin                                      1822                                                                              NH(CNH)H    1 Ph      CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                      1823                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                      1824                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                      1825                                                                              NH(CNH)H    1 Ph      Ph       (+)-pin                                      1826                                                                              NH(CNH)H    1 Ph      PhCH.sub.2                                                                              (+)-pin                                      1827                                                                              NH(CNH)H    1 Ph      Ph(CH.sub.2).sub.2                                                                      (+)-pin                                      1828                                                                              NH(CNH)H    1 Ph      3-NO.sub.2 -Ph                                                                          (+)-pin                                      1829                                                                              NH(CNH)H    1 Ph      4-NO.sub.2 -Ph                                                                          (+)-pin                                      1830                                                                              NH(CNH)H    1 Ph      3-CO.sub.2 H-Ph                                                                         (+)-pin                                      1831                                                                              NH(CNH)H    1 Ph      4-CO.sub.2 H-Ph                                                                         (+)-pin                                      1832                                                                              NH(CNH)H    1 Ph      3-CN.sub.4 H-Ph                                                                         (+)-pin                                      1833                                                                              NH(CNH)H    1 Ph      4-CN.sub.4 H-Ph                                                                         (+)-pin                                      1834                                                                              NH(CNH)H    1 Ph      3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      1835                                                                              NH(CNH)H    1 Ph      4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      1836                                                                              NH(CNH)H    1 Ph      H        OH, OH                                       1837                                                                              NH(CNH)H    1 Ph      Methyl   OH, OH                                       1838                                                                              NH(CNH)H    1 Ph      Ethyl    OH, OH                                       1839                                                                              NH(CNH)H    1 Ph      n-Propyl OH, OH                                       1840                                                                              NH(CNH)H    1 Ph      n-Butyl  OH, OH                                       1841                                                                              NH(CNH)H    1 Ph      CH.sub.2 SCH.sub.3                                                                      OH, OH                                       1842                                                                              NH(CNH)H    1 Ph      CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                       1843                                                                              NH(CNH)H    1 Ph      CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                       1844                                                                              NH(CNH)H    1 Ph      CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                       1845                                                                              NH(CNH)H    1 Ph      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                       1846                                                                              NH(CNH)H    1 Ph      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                       1847                                                                              NH(CNH)H    1 Ph      CH.sub.2 CN                                                                             OH, OH                                       1848                                                                              NH(CNH)H    1 Ph      CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                       1849                                                                              NH(CNH)H    1 Ph      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                       1850                                                                              NH(CNH)H    1 Ph      CF.sub.3 OH, OH                                       1851                                                                              NH(CNH)H    1 Ph      CF.sub.2 CF.sub.3                                                                       OH, OH                                       1852                                                                              NH(CNH)H    1 Ph      CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                       1853                                                                              NH(CNH)H    1 Ph      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                       1854                                                                              NH(CNH)H    1 Ph      F.sub.5 -Ph                                                                             OH, OH                                       1855                                                                              NH(CNH)H    1 Ph      CH.sub.2 CO.sub.2 H                                                                     OH, OH                                       1856                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                       1857                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                       1858                                                                              NH(CNH)H    1 Ph      CH.sub.2 CN.sub.4 H                                                                     OH, OH                                       1859                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                       1860                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                       1861                                                                              NH(CNH)H    1 Ph      CH.sub.2 NO.sub.2                                                                       OH, OH                                       1862                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                       1863                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                       1864                                                                              NH(CNH)H    1 Ph      CH.sub.2 OH                                                                             OH, OH                                       1865                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.2 OH                                                                     OH, OH                                       1866                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.3 OH                                                                     OH, OH                                       1867                                                                              NH(CNH)H    1 Ph      CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                       1868                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                       1869                                                                              NH(CNH)H    1 Ph      (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                       1870                                                                              NH(CNH)H    1 Ph      Ph       OH, OH                                       1871                                                                              NH(CNH)H    1 Ph      PhCH.sub.2                                                                              OH, OH                                       1872                                                                              NH(CNH)H    1 Ph      Ph(CH.sub.2).sub.2                                                                      OH, OH                                       1873                                                                              NH(CNH)H    1 Ph      3-NO.sub.2 -Ph                                                                          OH, OH                                       1874                                                                              NH(CNH)H    1 Ph      4-NO.sub.2 -Ph                                                                          OH, OH                                       1875                                                                              NH(CNH)H    1 Ph      3-CO.sub.2 H-Ph                                                                         OH, OH                                       1876                                                                              NH(CNH)H    1 Ph      4-CO.sub.2 H-Ph                                                                         OH, OH                                       1877                                                                              NH(CNH)H    1 Ph      3-CN.sub.4 H-Ph                                                                         OH, OH                                       1878                                                                              NH(CNH)H    1 Ph      4-CN.sub.4 H-Ph                                                                         OH, OH                                       1879                                                                              NH(CNH)H    1 Ph      3-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1880                                                                              NH(CNH)H    1 Ph      4-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1881                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             H        (+)-pin                                      1882                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             Methyl   (+)-pin                                      1883                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             Ethyl    (+)-pin                                      1884                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             n-Propyl (+)-pin                                      1885                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             n-Butyl  (+)-pin                                      1886                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 SCH.sub.3                                                                      (+)-pin                                      1887                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                      1888                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                      1889                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                      1890                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                      1891                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                      1892                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      1893                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                      1894                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                      1895                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CF.sub.3 (+)-pin                                      1896                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.3                                                                       (+)-pin                                      1897                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                      1898                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                      1899                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             F.sub.5 -Ph                                                                             (+)-pin                                      1900                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                      1901                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                      1902                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                      1903                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                      1904                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                      1905                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                      1906                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      1907                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                      1908                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                      1909                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 OH                                                                             (+)-pin                                      1910                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      1911                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 OH                                                                     (+)-pin                                      1912                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                      1913                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                      1914                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                      1915                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             Ph       (+)-pin                                      1916                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             PhCH.sub.2                                                                              (+)-pin                                      1917                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             Ph(CH.sub.2).sub.2                                                                      (+)-pin                                      1918                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             3-NO.sub.2 -Ph                                                                          (+)-pin                                      1919                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             4-NO.sub.2 -Ph                                                                          (+)-pin                                      1920                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             3-CO.sub.2 H-Ph                                                                         (+)-pin                                      1921                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             4-CO.sub.2 H-Ph                                                                         (+)-pin                                      1922                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             3-CN.sub.4 H-Ph                                                                         (+)-pin                                      1923                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             4-CN.sub.4 H-Ph                                                                         (+)-pin                                      1924                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      1925                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      1926                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             H        OH, OH                                       1927                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             Methyl   OH, OH                                       1928                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             Ethyl    OH, OH                                       1929                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             n-Propyl OH, OH                                       1930                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             n-Butyl  OH, OH                                       1931                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 SCH.sub.3                                                                      OH, OH                                       1932                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                       1933                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                       1934                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                       1935                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                       1936                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                       1937                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       1938                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                       1939                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                       1940                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CF.sub.3 OH, OH                                       1941                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.3                                                                       OH, OH                                       1942                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                       1943                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                       1944                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             F.sub.5 -Ph                                                                             OH, OH                                       1945                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 H                                                                     OH, OH                                       1946                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                       1947                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                       1948                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CN.sub.4 H                                                                     OH, OH                                       1949                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                       1950                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                       1951                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       1952                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                       1953                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                       1954                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 OH                                                                             OH, OH                                       1955                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       1956                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 OH                                                                     OH, OH                                       1957                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                       1958                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                       1959                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                       1960                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             Ph       OH, OH                                       1961                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             PhCH.sub.2                                                                              OH, OH                                       1962                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             Ph(CH.sub.2).sub.2                                                                      OH, OH                                       1963                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             3-NO.sub.2 -Ph                                                                          OH, OH                                       1964                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             4-NO.sub.2 -Ph                                                                          OH, OH                                       1965                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             3-CO.sub.2 H-Ph                                                                         OH, OH                                       1966                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             4-CO.sub.2 H-Ph                                                                         OH, OH                                       1967                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             3-CN.sub.4 H-Ph                                                                         OH, OH                                       1968                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             4-CN.sub.4 H-Ph                                                                         OH, OH                                       1969                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             3-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1970                                                                              NH(CNH)H    1 PhCH.sub.2                                                                             4-(HOCH.sub.2)-Ph                                                                       OH, OH                                       1971                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    H        (+)-pin                                      1972                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    Methyl   (+)-pin                                      1973                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    Ethyl    (+)-pin                                      1974                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    n-Propyl (+)-pin                                      1975                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    n-Butyl  (+)-pin                                      1976                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 SCH.sub.3                                                                      (+)-pin                                      1977                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                      1978                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                      1979                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                      1980                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                      1981                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                      1982                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN                                                                             (+)-pin                                      1983                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                      1984                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                      1985                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.3 (+)-pin                                      1986                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.3                                                                       (+)-pin                                      1987                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                      1988                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                      1989                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    F.sub.5 -Ph                                                                             (+)-pin                                      1990                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                      1991                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                      1992                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                      1993                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                      1994                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                      1995                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                      1996                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 NO.sub.2                                                                       (+)-pin                                      1997                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                      1998                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                      1999                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 OH                                                                             (+)-pin                                      2000                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      2001                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 OH                                                                     (+)-pin                                      2002                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                      2003                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                      2004                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                      2005                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    Ph       (+)-pin                                      2006                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    PhCH.sub.2                                                                              (+)-pin                                      2007                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    Ph(CH.sub.2).sub.2                                                                      (+)-pin                                      2008                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    3-NO.sub.2 -Ph                                                                          (+)-pin                                      2009                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    4-NO.sub.2 -Ph                                                                          (+)-pin                                      2010                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    3-CO.sub.2 H-Ph                                                                         (+)-pin                                      2011                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    4-CO.sub.2 H-Ph                                                                         (+)-pin                                      2012                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    3-CN.sub.4 H-Ph                                                                         (+)-pin                                      2013                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    4-CN.sub.4 H-Ph                                                                         (+)-pin                                      2014                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      2015                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                      2016                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    H        OH, OH                                       2017                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    Methyl   OH, OH                                       2018                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    Ethyl    OH, OH                                       2019                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    n-Propyl OH, OH                                       2020                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    n-Butyl  OH, OH                                       2021                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 SCH.sub.3                                                                      OH, OH                                       2022                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                       2023                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                       2024                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                       2025                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                       2026                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                       2027                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN                                                                             OH, OH                                       2028                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                       2029                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                       2030                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.3 OH, OH                                       2031                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.3                                                                       OH, OH                                       2032                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                       2033                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                       2034                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    F.sub.5 -Ph                                                                             OH, OH                                       2035                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 H                                                                     OH, OH                                       2036                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                       2037                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                       2038                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CN.sub.4 H                                                                     OH, OH                                       2039                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                       2040                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                       2041                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 NO.sub.2                                                                       OH, OH                                       2042                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                       2043                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                       2044                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 OH                                                                             OH, OH                                       2045                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 OH                                                                     OH, OH                                       2046                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 OH                                                                     OH, OH                                       2047                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                       2048                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                       2049                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                       2050                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    Ph       OH, OH                                       2051                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    PhCH.sub.2                                                                              OH, OH                                       2052                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    Ph(CH.sub.2).sub.2                                                                      OH, OH                                       2053                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    3-NO.sub.2 -Ph                                                                          OH, OH                                       2054                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    4-NO.sub.2 -Ph                                                                          OH, OH                                       2055                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    3-CO.sub.2 H-Ph                                                                         OH, OH                                       2056                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    4-CO.sub.2 H-Ph                                                                         OH, OH                                       2057                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    3-CN.sub.4 H-Ph                                                                         OH, OH                                       2058                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    4-CN.sub.4 H-Ph                                                                         OH, OH                                       2059                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    3-(HOCH.sub.2)-Ph                                                                       OH, OH                                       2060                                                                              NH(CNH)H    1 PhCH.sub.2 CH.sub.2                                                                    4-(HOCH.sub.2)-Ph                                                                       OH, OH                                       2061                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             3-NO.sub.2 Ph                                                                           (+)-pin CU                                   2062                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      PhCH.sub.2                                                                              (+)-pin                                      2063                                                                              NH(CNH)NH.sub.2                                                                            1 Ph      PhCH.sub.2 CH.sub.2                                                                     (+)-pin                                      2064                                                                              S(CNH)NH.sub.2                                                                             1 Ph      PhCH.sub.2                                                                              (+)-pin                                      2065                                                                              S(CNH)NH.sub.2                                                                             1 Ph      PhCH.sub.2 CH.sub.2                                                                     (+)-pin                                      2066                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin CN                                   2067                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2                                                                             CH.sub.2 CN.sub.4 H                                                                     (+)-pin CO                                   2068                                                                              CH.sub.2 NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                    CH.sub.2 OCH.sub.2 Ph                                                                   (+)-pin CT                                   __________________________________________________________________________      AG. Anal. calcd. for C.sub.32 H.sub.42 BN.sub.5 O.sub.3.0.7H.sub.2             O.17HCl: 6, 61.00; H, 7.21; Cl, 9.56 N, 11.11. Found: C, 60.93; H, 7.20;       Cl, 9.57 N, 11.55.                                                             AH. Anal. calcd. for C.sub.22 H.sub.28 BN.sub.5 O.sub.3.12H.sub.2              O.2.6HCl: C, 36.09; Cl., 12.59; N, 9.56. Found: C, 36.25; Cl, 12.52; N,        9.32.                                                                          AI. Anal. calcd. for C.sub.16 H.sub.24 BN.sub.5 O.sub.3.1.5H.sub.2             O.1.8HCl: C, 43.89; H, 6.63; Cl, 14.57; N, 16.06. Found: C, 44.01; H,          6.28; Cl, 14.21; N, 15.59.                                                     AJ. Anal. calcd. for C.sub.25 H.sub.34 BN.sub.5 O.sub.3.2H.sub.2 O.1.6HCl      C, 53.84; H, 7.16; Cl, 10.17; N, 12.56. Found: C, 53.71; H, 7.13; Cl,          10.25; N, 12.60.                                                               AK. MS (M+H).sup.+ : Calc. 480, Found 480.                                     AL. MS (M+H).sup.+ : Calc. 494, Found 494.                                     AM. MS (M+H).sup.+ : Calc. 522, Found 522.                                     AN MS (M+H).sup.+ : Calc. 540, Found 540.                                      AO. MS (M+H).sup.+ : Calc. 510, Found 510.                                     AP. MS (M+H).sup.+ : Calc. 600, Found 600.                                     AQ. MS (M+H).sup.+ : Calc. 556, Found 556.                                     AR. MS (M+H).sup.+ : Calc. 570, Found 570.                                     AS. MS (M+H).sup.+ : Calc. 601, Found 601.                                     AT. MS (M+H).sup.+ : Calc. 598, FOund 598.                                     AU. MS (M+H).sup.+ : Calc. 629, Found 629.                                     AV. MS (M+H).sup.+ : Calc. 422, Found 422.                                     AW. MS (M+H).sup.+ : Calc. 538, Found 538.                                     AX. MS (M+H).sup.+ : Calc. 494, Found 494.                                     AY. MS (M+H).sup.+ : Calc. 598, Found 598.                                     AZ. MS (M+H).sup.+ : Calc. 360, Found 360.                                     CN. MS (M+H).sup.+ : Calc. 519, Found 519.                                     CO. MS (M+H).sup.+ : Calc. 562, Found 562.                                     CP. MS (M+H).sup.+ : Calc. 552, Found 552.                                     CQ. MS (M+H).sup.+ : Calc. 571, Found 571.                                     CR. MS (M+H).sup.+ : Calc. 520, Found 520.                                     CS. MS (M+H).sup.+ : Calc. 524, Found 524.                                     CT. MS (M+H).sup.+ : Calc. 614, Found 614.                                     CU. MS (M+H).sup.+ : Calc. 571, Found 571.                               

                                      TABLE 15                                     __________________________________________________________________________      ##STR110##                                                                                                       Phys.                                       Ex X         m R.sup.13                                                                             R.sup.14 Y.sup.1 Y.sup.2                                                                     Data                                        __________________________________________________________________________     2073                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    H        (+)-pin                                                                             BW                                          2074                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    Methyl   (+)-pin                                                                             BX                                          2075                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    Ethyl    (+)-pin                                          2076                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    n-Propyl (+)-pin                                          2077                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    n-Butyl  (+)-pin                                          2078                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 SCH.sub.3                                                                      (+)-pin                                          2079                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                          2080                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                          2081                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                          2082                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                          2083                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                          2084                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CN                                                                             (+)-pin                                          2085                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                          2086                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                          2087                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CF.sub.3 (+)-pin                                          2088                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CF.sub.2 CF.sub.3                                                                       (+)-pin                                          2089                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                          2090                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                          2091                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    F.sub.5 -Ph                                                                             (+)-pin                                          2092                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                          2093                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                          2094                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                          2095                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                          2096                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                          2097                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                          2098                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 NO.sub.2                                                                       (+)-pin                                          2099                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                          2100                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                          2101                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 OH                                                                             (+)-pin                                          2102                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 OH                                                                     (+)-pin                                          2103                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 OH                                                                     (+)-pin                                          2104                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                          2105                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                          2106                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                          2107                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    3-NO.sub.2 -Ph                                                                          (+)-pin                                          2108                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    4-NO.sub.2 -Ph                                                                          (+)-pin                                          2109                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    3-CO.sub.2 H-Ph                                                                         (+)-pin                                          2110                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    4-CO.sub.2 H-Ph                                                                         (+)-pin                                          2111                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    3-CN.sub.4 H-Ph                                                                         (+)-pin                                          2112                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    4-CN.sub.4 H-Ph                                                                         (+)-pin                                          2113                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2114                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2115                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    H        (+)-pin                                          2116                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    Methyl   (+)-pin                                          2117                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    Ethyl    (+)-pin                                          2118                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    n-Propyl (+)-pin                                          2119                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    n-Butyl  (+)-pin                                          2120                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 SCH.sub.3                                                                      (+)-pin                                          2121                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                          2122                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                          2123                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                          2124                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                          2125                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                          2126                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CN                                                                             (+)-pin                                          2127                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                          2128                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                          2129                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.3 (+)-pin                                          2130                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.3                                                                       (+)-pin                                          2131                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                          2132                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                          2133                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    F.sub.5 -Ph                                                                             (+)-pin                                          2134                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                          2135                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                          2136                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                          2137                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                          2138                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                          2139                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                          2140                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 NO.sub.2                                                                       (+)-pin                                          2141                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                          2142                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                          2143                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 OH                                                                             (+)-pin                                          2144                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 OH                                                                     (+)-pin                                          2145                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 OH                                                                     (+)-pin                                          2146                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                          2147                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                          2148                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                          2149                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-NO.sub.2 -Ph                                                                          (+)-pin                                          2150                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-NO.sub.2 -Ph                                                                          (+)-pin                                          2151                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-CO.sub.2 H-Ph                                                                         (+)-pin                                          2152                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-CO.sub.2 H-Ph                                                                         (+)-pin                                          2153                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-CN.sub.4 H-Ph                                                                         (+)-pin                                          2154                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-CN.sub.4 H-Ph                                                                         (+)-pin                                          2155                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2156                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2157                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    H        OH, OH                                           2158                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    Methyl   OH, OH                                           2159                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    Ethyl    OH, OH                                           2160                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    n-Propyl OH, OH                                           2161                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    n-Butyl  OH, OH                                           2162                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 SCH.sub.3                                                                      OH, OH                                           2163                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                           2164                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                           2165                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                           2166                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                           2167                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                           2168                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CN                                                                             OH, OH                                           2169                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                           2170                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                           2171                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CF.sub.3 OH, OH                                           2172                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CF.sub.2 CF.sub.3                                                                       OH, OH                                           2173                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                           2174                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                           2175                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    F.sub.5 -Ph                                                                             OH, OH                                           2176                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CO.sub.2 H                                                                     OH, OH                                           2177                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                           2178                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                           2179                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CN.sub.4 H                                                                     OH, OH                                           2180                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                           2181                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                           2182                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 NO.sub.2                                                                       OH, OH                                           2183                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                           2184                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                           2185                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 OH                                                                             OH, OH                                           2186                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 OH                                                                     OH, OH                                           2187                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 OH                                                                     OH, OH                                           2188                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                           2189                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                           2190                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                           2191                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    3-NO.sub.2 -Ph                                                                          OH, OH                                           2192                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    4-NO.sub.2 -Ph                                                                          OH, OH                                           2193                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    3-CO.sub.2 H-Ph                                                                         OH, OH                                           2194                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    4-CO.sub.2 H-Ph                                                                         OH, OH                                           2195                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    3-CN.sub.4 H-Ph                                                                         OH, OH                                           2196                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    4-CN.sub.4 H-Ph                                                                         OH, OH                                           2197                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    3-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2198                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    4-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2199                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    H        OH, OH                                           2200                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    Methyl   OH, OH                                           2201                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    Ethyl    OH, OH                                           2202                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    n-Propyl OH, OH                                           2203                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    n-Butyl  OH, OH                                           2204                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 SCH.sub.3                                                                      OH, OH                                           2205                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                           2206                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                           2207                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                           2208                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                           2209                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                           2210                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CN                                                                             OH, OH                                           2211                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                           2212                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                           2213                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.3 OH, OH                                           2214                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.3                                                                       OH, OH                                           2215                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                           2216                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                           2217                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    F.sub.5 -Ph                                                                             OH, OH                                           2218                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CO.sub.2 H                                                                     OH, OH                                           2219                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                           2220                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                           2221                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CN.sub.4 H                                                                     OH, OH                                           2222                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                           2223                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                           2224                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 NO.sub.2                                                                       OH, OH                                           2225                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                           2226                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                           2227                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 OH                                                                             OH, OH                                           2228                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 OH                                                                     OH, OH                                           2229                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 OH                                                                     OH, OH                                           2230                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                           2231                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                           2232                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                           2233                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-NO.sub.2 -Ph                                                                          OH, OH                                           2234                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-NO.sub.2 -Ph                                                                          OH, OH                                           2235                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-CO.sub.2 H-Ph                                                                         OH, OH                                           2236                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-CO.sub.2 H-Ph                                                                         OH, OH                                           2237                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-CN.sub.4 H-Ph                                                                         OH, OH                                           2238                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-CN.sub.4 H-Ph                                                                         OH, OH                                           2239                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2240                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2241                                                                              S(CNH)NH.sub.2                                                                           1 Ph    H        (+)-pin                                          2242                                                                              S(CNH)NH.sub.2                                                                           1 Ph    Methyl   (+)-pin                                          2243                                                                              S(CNH)NH.sub.2                                                                           1 Ph    Ethyl    (+)-pin                                          2244                                                                              S(CNH)NH.sub.2                                                                           1 Ph    n-Propyl (+)-pin                                          2245                                                                              S(CNH)NH.sub.2                                                                           1 Ph    n-Butyl  (+)-pin                                          2246                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 SCH.sub.3                                                                      (+)-pin                                          2247                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                          2248                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                          2249                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                          2250                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                          2251                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                          2252                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CN                                                                             (+)-pin                                          2253                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                          2254                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                          2255                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CF.sub.3 (+)-pin                                          2256                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CF.sub.2 CF.sub.3                                                                       (+)-pin                                          2257                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                          2258                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                          2259                                                                              S(CNH)NH.sub.2                                                                           1 Ph    F.sub.5 -Ph                                                                             (+)-pin                                          2260                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                          2261                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                          2262                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                          2263                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                          2264                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                          2265                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                          2266                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 NO.sub.2                                                                       (+)-pin                                          2267                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                          2268                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                          2269                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 OH                                                                             (+)-pin                                          2270                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 OH                                                                     (+)-pin                                          2271                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 OH                                                                     (+)-pin                                          2272                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                          2273                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                          2274                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                          2275                                                                              S(CNH)NH.sub.2                                                                           1 Ph    3-NO.sub.2 -Ph                                                                          (+)-pin                                          2276                                                                              S(CNH)NH.sub.2                                                                           1 Ph    4-NO.sub.2 -Ph                                                                          (+)-pin                                          2277                                                                              S(CNH)NH.sub.2                                                                           1 Ph    3-CO.sub.2 H-Ph                                                                         (+)-pin                                          2278                                                                              S(CNH)NH.sub.2                                                                           1 Ph    4-CO.sub.2 H-Ph                                                                         (+)-pin                                          2279                                                                              S(CNH)NH.sub.2                                                                           1 Ph    3-CN.sub.4 H-Ph                                                                         (+)-pin                                          2280                                                                              S(CNH)NH.sub.2                                                                           1 Ph    4-CN.sub.4 H-Ph                                                                         (+)-pin                                          2281                                                                              S(CNH)NH.sub.2                                                                           1 Ph    3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2282                                                                              S(CNH)NH.sub.2                                                                           1 Ph    4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2283                                                                              S(CNH)NH.sub.2                                                                           1 Ph    H        OH, OH                                           2284                                                                              S(CNH)NH.sub.2                                                                           1 Ph    Methyl   OH, OH                                           2285                                                                              S(CNH)NH.sub.2                                                                           1 Ph    Ethyl    OH, OH                                           2286                                                                              S(CNH)NH.sub.2                                                                           1 Ph    n-Propyl OH, OH                                           2287                                                                              S(CNH)NH.sub.2                                                                           1 Ph    n-Butyl  OH, OH                                           2288                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 SCH.sub.3                                                                      OH, OH                                           2289                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                           2290                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                           2291                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                           2292                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                           2293                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                           2294                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CN                                                                             OH, OH                                           2295                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                           2296                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                           2297                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CF.sub.3 OH, OH                                           2298                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CF.sub.2 CF.sub.3                                                                       OH, OH                                           2299                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                           2300                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                           2301                                                                              S(CNH)NH.sub.2                                                                           1 Ph    F.sub.5 -Ph                                                                             OH, OH                                           2302                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CO.sub.2 H                                                                     OH, OH                                           2303                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                           2304                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                           2305                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CN.sub.4 H                                                                     OH, OH                                           2306                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                           2307                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                           2308                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 NO.sub.2                                                                       OH, OH                                           2309                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                           2310                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                           2311                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 OH                                                                             OH, OH                                           2312                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 OH                                                                     OH, OH                                           2313                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 OH                                                                     OH, OH                                           2314                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                           2315                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                           2316                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                           2317                                                                              S(CNH)NH.sub.2                                                                           1 Ph    3-NO.sub.2 -Ph                                                                          OH, OH                                           2318                                                                              S(CNH)NH.sub.2                                                                           1 Ph    4-NO.sub.2 -Ph                                                                          OH, OH                                           2319                                                                              S(CNH)NH.sub.2                                                                           1 Ph    3-CO.sub.2 H-Ph                                                                         OH, OH                                           2320                                                                              S(CNH)NH.sub.2                                                                           1 Ph    4-CO.sub.2 H-Ph                                                                         OH, OH                                           2321                                                                              S(CNH)NH.sub.2                                                                           1 Ph    3-CN.sub.4 H-Ph                                                                         OH, OH                                           2322                                                                              S(CNH)NH.sub.2                                                                           1 Ph    4-CN.sub.4 H-Ph                                                                         OH, OH                                           2323                                                                              S(CNH)NH.sub.2                                                                           1 Ph    3-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2324                                                                              S(CNH)NH.sub.2                                                                           1 Ph    4-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2325                                                                              CH.sub.2 NH.sub.2                                                                        2 Ph    H        (+)-pin                                          2326                                                                              CH.sub.2 NH.sub.2                                                                        2 Ph    H        OH, OH                                           2327                                                                              OMe       1 Ph    H        (+)-pin                                          2328                                                                              OMe       1 Ph    Methyl   (+)-pin                                          2329                                                                              OMe       1 Ph    Ethyl    (+)-pin                                          2330                                                                              OMe       1 Ph    n-Propyl (+)-pin                                          2331                                                                              OMe       1 Ph    n-Butyl  (+)-pin                                          2332                                                                              OMe       1 Ph    CH.sub.2 SCH.sub.3                                                                      (+)-pin                                          2333                                                                              OMe       1 Ph    CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                          2334                                                                              OMe       1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                          2335                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                          2336                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                          2337                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                          2338                                                                              OMe       1 Ph    CH.sub.2 CN                                                                             (+)-pin                                          2339                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                          2340                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                          2341                                                                              OMe       1 Ph    CF.sub.3 (+)-pin                                          2342                                                                              OMe       1 Ph    CF.sub.2 CF.sub.3                                                                       (+)-pin                                          2343                                                                              OMe       1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                          2344                                                                              OMe       1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                          2345                                                                              OMe       1 Ph    F.sub.5 -Ph                                                                             (+)-pin                                          2346                                                                              OMe       1 Ph    CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                          2347                                                                              OMe       1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                          2348                                                                              OMe       1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                          2349                                                                              OMe       1 Ph    CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                          2350                                                                              OMe       1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                          2351                                                                              OMe       1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                          2352                                                                              OMe       1 Ph    CH.sub.2 NO.sub.2                                                                       (+)-pin                                          2353                                                                              OMe       1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                          2354                                                                              OMe       1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                          2355                                                                              OMe       1 Ph    CH.sub.2 OH                                                                             (+)-pin                                          2356                                                                              OMe       1 Ph    (CH.sub.2).sub.2 OH                                                                     (+)-pin                                          2357                                                                              OMe       1 Ph    (CH.sub.2).sub.3 OH                                                                     (+)-pin                                          2358                                                                              OMe       1 Ph    CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                          2359                                                                              OMe       1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                          2360                                                                              OMe       1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                          2361                                                                              OMe       1 Ph    3-NO.sub.2 -Ph                                                                          (+)-pin                                          2362                                                                              OMe       1 Ph    4-NO.sub.2 -Ph                                                                          (+)-pin                                          2363                                                                              OMe       1 Ph    3-CO.sub.2 H-Ph                                                                         (+)-pin                                          2364                                                                              OMe       1 Ph    4-CO.sub.2 H-Ph                                                                         (+)-pin                                          2365                                                                              OMe       1 Ph    3-CN.sub.4 H-Ph                                                                         (+)-pin                                          2366                                                                              OMe       1 Ph    4-CN.sub.4 H-Ph                                                                         (+)-pin                                          2367                                                                              OMe       1 Ph    3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2368                                                                              OMe       1 Ph    4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2369                                                                              OMe       1 Ph    H        OH, OH                                           2370                                                                              OMe       1 Ph    Methyl   OH, OH                                           2371                                                                              OMe       1 Ph    Ethyl    OH, OH                                           2372                                                                              OMe       1 Ph    n-Propyl OH, OH                                           2373                                                                              OMe       1 Ph    n-Butyl  OH, OH                                           2374                                                                              OMe       1 Ph    CH.sub.2 SCH.sub.3                                                                      OH, OH                                           2375                                                                              OMe       1 Ph    CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                           2376                                                                              OMe       1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                           2377                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                           2378                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                           2379                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                           2380                                                                              OMe       1 Ph    CH.sub.2 CN                                                                             OH, OH                                           2381                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                           2382                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                           2383                                                                              OMe       1 Ph    CF.sub.3 OH, OH                                           2384                                                                              OMe       1 Ph    CF.sub.2 CF.sub.3                                                                       OH, OH                                           2385                                                                              OMe       1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                           2386                                                                              OMe       1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                           2387                                                                              OMe       1 Ph    F.sub.5 -Ph                                                                             OH, OH                                           2388                                                                              OMe       1 Ph    CH.sub.2 CO.sub.2 H                                                                     OH, OH                                           2389                                                                              OMe       1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                           2390                                                                              OMe       1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                           2391                                                                              OMe       1 Ph    CH.sub.2 CN.sub.4 H                                                                     OH, OH                                           2392                                                                              OMe       1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                           2393                                                                              OMe       1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                           2394                                                                              OMe       1 Ph    CH.sub.2 NO.sub.2                                                                       OH, OH                                           2395                                                                              OMe       1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                           2396                                                                              OMe       1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                           2397                                                                              OMe       1 Ph    CH.sub.2 OH                                                                             OH, OH                                           2398                                                                              OMe       1 Ph    (CH.sub.2).sub.2 OH                                                                     OH, OH                                           2399                                                                              OMe       1 Ph    (CH.sub.2).sub.3 OH                                                                     OH, OH                                           2400                                                                              OMe       1 Ph    CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                           2401                                                                              OMe       1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                           2402                                                                              OMe       1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                           2403                                                                              OMe       1 Ph    3-NO.sub.2 -Ph                                                                          OH, OH                                           2404                                                                              OMe       1 Ph    4-NO.sub.2 -Ph                                                                          OH, OH                                           2405                                                                              OMe       1 Ph    3-CO.sub.2 H-Ph                                                                         OH, OH                                           2406                                                                              OMe       1 Ph    4-CO.sub.2 H-Ph                                                                         OH, OH                                           2407                                                                              OMe       1 Ph    3-CN.sub.4 H-Ph                                                                         OH, OH                                           2408                                                                              OMe       1 Ph    4-CN.sub.4 H-Ph                                                                         OH, OH                                           2409                                                                              OMe       1 Ph    3-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2410                                                                              OMe       1 Ph    4-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2411                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           H        (+)-pin                                                                             BA                                          2412                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           Methyl   (+)-pin                                                                             BC                                          2413                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           Ethyl    (+)-pin                                          2414                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           n-Propyl (+)-pin                                                                             BD                                          2415                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           n-Butyl  (+)-pin                                          2416                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                      (+)-pin                                                                             BE                                          2417                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                          2418                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                          2419                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                          2420                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                          2421                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                          2422                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                             (+)-pin                                                                             BF                                          2423                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                          2424                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                          2425                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CF.sub.3 (+)-pin                                          2426                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                       (+)-pin                                          2427                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                          2428                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                          2429                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           F.sub.5 -Ph                                                                             (+)-pin                                          2430                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                                                             BG                                          2431                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                          2432                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                          2433                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                          2434                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                          2435                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                          2436                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                       (+)-pin                                          2437                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                          2438                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                          2439                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                             (+)-pin                                                                             CV                                          2440                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 OCH.sub.2 Ph                                                                   (+)-pin                                                                             CW                                          2441                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                     (+)-pin                                          2442                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                     (+)-pin                                          2443                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                          2444                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                                                             CX                                          2445                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                          2446                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           Ph       (+)-pin                                          2447                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           PhCH.sub.2                                                                              (+)-pin                                          2448                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           3-NO.sub.2 -Ph                                                                          (+)-pin                                          2449                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           4-NO.sub.2 -Ph                                                                          (+)-pin                                          2450                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           3-CO.sub.2 H-Ph                                                                         (+)-pin                                          2451                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           4-CO.sub.2 H-Ph                                                                         (+)-pin                                          2452                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           3-CN.sub.4 H-Ph                                                                         (+)-pin                                          2453                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           4-CN.sub.4 H-Ph                                                                         (+)-pin                                          2454                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2455                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2456                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           H        (+)-pin                                          2457                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           Methyl   (+)-pin                                          2458                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           Ethyl    (+)-pin                                          2459                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           n-Propyl (+)-pin                                          2460                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           n-Butyl  (+)-pin                                          2461                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                      (+)-pin                                          2462                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                          2463                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                          2464                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                          2465                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                          2466                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                          2467                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                             (+)-pin                                          2468                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                          2469                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                          2470                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.3 (+)-pin                                          2471                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                       (+)-pin                                          2472                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                          2473                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                          2474                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           F.sub.5 -Ph                                                                             (+)-pin                                          2475                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                          2476                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                          2477                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                          2478                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                          2479                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                          2480                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                          2481                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                       (+)-pin                                          2482                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                          2483                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                          2484                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                             (+)-pin                                          2485                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                     (+)-pin                                          2486                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                     (+)-pin                                          2487                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                          2488                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                          2489                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                          2490                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           Ph       (+)-pin                                          2491                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-NO.sub.2 -Ph                                                                          (+)-pin                                                                             CY                                          2492                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-NO.sub.2 -Ph                                                                          (+)-pin                                          2493                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-CO.sub.2 H-Ph                                                                         (+)-pin                                          2494                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-CO.sub.2 H-Ph                                                                         (+)-pin                                          2495                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-CN.sub.4 H-Ph                                                                         (+)-pin                                          2496                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-CN.sub.4 H-Ph                                                                         (+)-pin                                          2497                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2498                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2499                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           H        OH, OH                                                                              BH                                          2500                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           Methyl   OH, OH                                           2501                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           Ethyl    OH, OH                                           2502                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           n-Propyl OH, OH                                           2503                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           n-Butyl  OH, OH                                           2504                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                      OH, OH                                           2505                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                           2506                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                           2507                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                           2508                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                           2509                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                           2510                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                             OH, OH                                           2511                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                           2512                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                           2513                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CF.sub.3 OH, OH                                           2514                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                       OH, OH                                           2515                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                           2516                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                           2517                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           F.sub.5 -Ph                                                                             OH, OH                                           2518                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                     OH, OH                                           2519                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                           2520                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                           2521                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                     OH, OH                                           2522                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                           2523                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                           2524                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                       OH, OH                                           2525                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                           2526                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                           2527                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                             OH, OH                                           2528                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                     OH, OH                                           2529                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                     OH, OH                                           2530                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                           2531                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                           2532                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                           2533                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           Ph       OH, OH                                           2534                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           3-NO.sub.2 -Ph                                                                          OH, OH                                           2535                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           4-NO.sub.2 -Ph                                                                          OH, OH                                           2536                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           3-CO.sub.2 H-Ph                                                                         OH, OH                                           2537                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           4-CO.sub.2 H-Ph                                                                         OH, OH                                           2538                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           3-CN.sub.4 H-Ph                                                                         OH, OH                                           2539                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           4-CN.sub.4 H-Ph                                                                         OH, OH                                           2540                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           3-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2541                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           4-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2542                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           H        OH, OH                                           2543                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           Methyl   OH, OH                                           2544                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           Ethyl    OH, OH                                           2545                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           n-Propyl OH, OH                                           2546                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           n-Butyl  OH, OH                                           2547                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                      OH, OH                                           2548                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                           2549                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                           2550                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                           2551                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                           2552                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                           2553                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                             OH, OH                                           2554                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                           2555                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                           2556                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.3 OH, OH                                           2557                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                       OH, OH                                           2558                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                           2559                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                           2560                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           F.sub.5 -Ph                                                                             OH, OH                                           2561                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                     OH, OH                                           2562                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                           2563                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                           2564                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                     OH, OH                                           2565                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                           2566                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                           2567                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                       OH, OH                                           2568                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                           2569                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                           2570                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                             OH, OH                                           2571                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                     OH, OH                                           2572                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                     OH, OH                                           2573                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                           2574                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                           2575                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                           2576                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-NO.sub.2 -Ph                                                                          OH, OH                                           2577                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-NO.sub.2 -Ph                                                                          OH, OH                                           2578                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-CO.sub.2 H-Ph                                                                         OH, OH                                           2579                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-CO.sub.2 H-Ph                                                                         OH, OH                                           2580                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-CN.sub.4 H-Ph                                                                         OH, OH                                           2581                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-CN.sub.4 H-Ph                                                                         OH, OH                                           2582                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2583                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2584                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           H        (+)-pin                                          2585                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           Methyl   (+)-pin                                          2586                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           Ethyl    (+)-pin                                          2587                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           n-Propyl (+)-pin                                          2588                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           n-Butyl  (+)-pin                                          2589                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                      (+)-pin                                          2590                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                          2591                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                          2592                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                          2593                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                          2594                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                          2595                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                             (+)-pin                                          2596                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                          2597                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                          2598                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CF.sub.3 (+)-pin                                          2599                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                       (+)-pin                                          2600                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                          2601                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                          2602                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           F.sub.5 -Ph                                                                             (+)-pin                                          2603                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                          2604                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                          2605                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                          2606                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                          2607                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                          2608                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                          2609                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                       (+)-pin                                          2610                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                          2611                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                          2612                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                             (+)-pin                                          2613                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                     (+)-pin                                          2614                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                     (+)-pin                                          2615                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                          2616                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                          2617                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                          2618                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           3-NO.sub.2 -Ph                                                                          (+)-pin                                          2619                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           4-NO.sub.2 -Ph                                                                          (+)-pin                                          2620                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           3-CO.sub.2 H-Ph                                                                         (+)-pin                                          2621                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           4-CO.sub.2 H-Ph                                                                         (+)-pin                                          2622                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           3-CN.sub.4 H-Ph                                                                         (+)-pin                                          2623                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           4-CN.sub.4 H-Ph                                                                         (+)-pin                                          2624                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2625                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2626                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           H        OH, OH                                           2627                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           Methyl   OH, OH                                           2628                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           Ethyl    OH, OH                                           2629                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           n-Propyl OH, OH                                           2630                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           n-Butyl  OH, OH                                           2631                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                      OH, OH                                           2632                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                           2633                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                           2634                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                           2635                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                           2636                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                           2637                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                             OH, OH                                           2638                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                           2639                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                           2640                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CF.sub.3 OH, OH                                           2641                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                       OH, OH                                           2642                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                           2643                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                           2644                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           F.sub.5 -Ph                                                                             OH, OH                                           2645                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                     OH, OH                                           2646                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                           2647                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                           2648                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                     OH, OH                                           2649                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                           2650                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                           2651                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                       OH, OH                                           2652                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                           2653                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                           2654                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                             OH, OH                                           2655                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                     OH, OH                                           2656                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                     OH, OH                                           2657                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                           2658                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                           2659                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                           2660                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           3-NO.sub.2 -Ph                                                                          OH, OH                                           2661                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           4-NO.sub.2 -Ph                                                                          OH, OH                                           2662                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           3-CO.sub.2 H-Ph                                                                         OH, OH                                           2663                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           4-CO.sub.2 H-Ph                                                                         OH, OH                                           2664                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           3-CN.sub.4 H-Ph                                                                         OH, OH                                           2665                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           4-CN.sub.4 H-Ph                                                                         OH, OH                                           2666                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           3-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2667                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           4-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2668                                                                              OMe       1 PhCH.sub.2                                                                           H        (+)-pin                                          2669                                                                              OMe       1 PhCH.sub.2                                                                           Methyl   (+)-pin                                          2670                                                                              OMe       1 PhCH.sub.2                                                                           Ethyl    (+)-pin                                          2671                                                                              OMe       1 PhCH.sub.2                                                                           n-Propyl (+)-pin                                          2672                                                                              OMe       1 PhCH.sub.2                                                                           n-Butyl  (+)-pin                                          2673                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                      (+)-pin                                          2674                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                          2675                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                          2676                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                          2677                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                          2678                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                          2679                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                             (+)-pin                                          2680                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                          2681                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                          2682                                                                              OMe       1 PhCH.sub.2                                                                           CF.sub.3 (+)-pin                                          2683                                                                              OMe       1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                       (+)-pin                                          2684                                                                              OMe       1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                          2685                                                                              OMe       1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                          2686                                                                              OMe       1 PhCH.sub.2                                                                           F.sub.5 -Ph                                                                             (+)-pin                                          2687                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                          2688                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                          2689                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                          2690                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                          2691                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                          2692                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                          2693                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                       (+)-pin                                          2694                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                          2695                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                          2696                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                             (+)-pin                                          2697                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                     (+)-pin                                          2698                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                     (+)-pin                                          2699                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                          2700                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                          2701                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                          2702                                                                              OMe       1 PhCH.sub.2                                                                           3-NO.sub.2 -Ph                                                                          (+)-pin                                          2703                                                                              OMe       1 PhCH.sub.2                                                                           4-NO.sub.2 -Ph                                                                          (+)-pin                                          2704                                                                              OMe       1 PhCH.sub.2                                                                           3-CO.sub.2 H-Ph                                                                         (+)-pin                                          2705                                                                              OMe       1 PhCH.sub.2                                                                           4-CO.sub.2 H-Ph                                                                         (+)-pin                                          2706                                                                              OMe       1 PhCH.sub.2                                                                           3-CN.sub.4 H-Ph                                                                         (+)-pin                                          2707                                                                              OMe       1 PhCH.sub.2                                                                           4-CN.sub.4 H-Ph                                                                         (+)-pin                                          2708                                                                              OMe       1 PhCH.sub.2                                                                           3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2709                                                                              OMe       1 PhCH.sub.2                                                                           4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2710                                                                              OMe       1 PhCH.sub.2                                                                           H        OH, OH                                           2711                                                                              OMe       1 PhCH.sub.2                                                                           Methyl   OH, OH                                           2712                                                                              OMe       1 PhCH.sub.2                                                                           Ethyl    OH, OH                                           2713                                                                              OMe       1 PhCH.sub.2                                                                           n-Propyl OH, OH                                           2714                                                                              OMe       1 PhCH.sub.2                                                                           n-Butyl  OH, OH                                           2715                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                      OH, OH                                           2716                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                           2717                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                           2718                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                           2719                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                           2720                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                           2721                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                             OH, OH                                           2722                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                           2723                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                           2724                                                                              OMe       1 PhCH.sub.2                                                                           CF.sub.3 OH, OH                                           2725                                                                              OMe       1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                       OH, OH                                           2726                                                                              OMe       1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                           2727                                                                              OMe       1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                           2728                                                                              OMe       1 PhCH.sub.2                                                                           F.sub.5 -Ph                                                                             OH, OH                                           2729                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                     OH, OH                                           2730                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                           2731                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                           2732                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                     OH, OH                                           2733                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                           2734                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                           2735                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                       OH, OH                                           2736                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                           2737                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                           2738                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                             OH, OH                                           2739                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                     OH, OH                                           2740                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                     OH, OH                                           2741                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                           2742                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                           2743                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                           2744                                                                              OMe       1 PhCH.sub.2                                                                           3-NO.sub.2 -Ph                                                                          OH, OH                                           2745                                                                              OMe       1 PhCH.sub.2                                                                           4-NO.sub.2 -Ph                                                                          OH, OH                                           2746                                                                              OMe       1 PhCH.sub.2                                                                           3-CO.sub.2 H-Ph                                                                         OH, OH                                           2747                                                                              OMe       1 PhCH.sub.2                                                                           4-CO.sub.2 H-Ph                                                                         OH, OH                                           2748                                                                              OMe       1 PhCH.sub.2                                                                           3-CN.sub.4 H-Ph                                                                         OH, OH                                           2749                                                                              OMe       1 PhCH.sub.2                                                                           4-CN.sub.4 H-Ph                                                                         OH, OH                                           2750                                                                              OMe       1 PhCH.sub.2                                                                           3-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2751                                                                              OMe       1 PhCH.sub.2                                                                           4-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2752                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  H        (+)-pin                                                                             BI                                          2753                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  Methyl   (+)-pin                                          2754                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  Ethyl    (+)-pin                                          2755                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl (+)-pin                                          2756                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl  (+)-pin                                          2757                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                      (+)-pin                                          2758                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                          2759                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                          2760                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                          2761                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                          2762                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                          2763                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                             (+)-pin                                          2764                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                          2765                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                          2766                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3 (+)-pin                                          2767                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                       (+)-pin                                          2768                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                          2769                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                          2770                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 -Ph                                                                             (+)-pin                                          2771                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                          2772                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                          2773                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                          2774                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                          2775                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                          2776                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                          2777                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                       (+)-pin                                          2778                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                          2779                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                          2780                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                             (+)-pin                                                                             CZ                                          2781                                                                              CH.sub.2 NH.sub.2                                                                        1 CH.sub.2                                                                             CH.sub.2 OCH.sub.2 Ph                                                                   (+)-pin                                                                             DA                                          2782                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                     (+)-pin                                          2783                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                     (+)-pin                                          2784                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                          2785                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                          2786                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                          2787                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 -Ph                                                                          (+)-pin                                          2788                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 -Ph                                                                          (+)-pin                                          2789                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 H-Ph                                                                         (+)-pin                                          2790                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 H-Ph                                                                         (+)-pin                                          2791                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 H-Ph                                                                         (+)-pin                                          2792                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 H-Ph                                                                         (+)-pin                                          2793                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2794                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2795                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  H        (+)-pin                                          2796                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  Methyl   (+)-pin                                          2797                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  Ethyl    (+)-pin                                          2798                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl (+)-pin                                          2799                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl  (+)-pin                                          2800                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                      (+)-pin                                          2801                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                          2802                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                          2803                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                          2804                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                          2805                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                          2806                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                             (+)-pin                                          2807                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                          2808                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                          2809                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3 (+)-pin                                          2810                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                       (+)-pin                                          2811                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                          2812                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                          2813                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 -Ph                                                                             (+)-pin                                          2814                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                          2815                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                          2816                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                          2817                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                          2818                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                          2819                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                          2820                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                       (+)-pin                                          2821                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                          2822                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                          2823                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                             (+)-pin                                          2824                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                     (+)-pin                                          2825                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                     (+)-pin                                          2826                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                          2827                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                          2828                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                          2829                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 -Ph                                                                          (+)-pin                                          2830                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 -Ph                                                                          (+)-pin                                          2831                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 H-Ph                                                                         (+)-pin                                          2832                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 H-Ph                                                                         (+)-pin                                          2833                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 H-Ph                                                                         (+)-pin                                          2834                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 H-Ph                                                                         (+)-pin                                          2835                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2836                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2837                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  H        OH, OH                                                                              BJ                                          2838                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  Methyl   OH, OH                                           2839                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  Ethyl    OH, OH                                           2840                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl OH, OH                                           2841                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl  OH, OH                                           2842                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                      OH, OH                                           2843                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                           2844                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                           2845                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                           2846                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                           2847                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                           2848                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                             OH, OH                                           2849                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                           2850                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                           2851                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3 OH, OH                                           2852                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                       OH, OH                                           2853                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                           2854                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                           2855                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 -Ph                                                                             OH, OH                                           2856                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                     OH, OH                                           2857                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                           2858                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                           2859                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                     OH, OH                                           2860                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                           2861                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                           2862                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                       OH, OH                                           2863                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                           2864                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                           2865                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                             OH, OH                                           2866                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                     OH, OH                                           2867                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                     OH, OH                                           2868                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                           2869                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                           2870                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                           2871                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 -Ph                                                                          OH, OH                                           2872                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 -Ph                                                                          OH, OH                                           2873                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 H-Ph                                                                         OH, OH                                           2874                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 H-Ph                                                                         OH, OH                                           2875                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 H-Ph                                                                         OH, OH                                           2876                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 H-Ph                                                                         OH, OH                                           2877                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2878                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2879                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  H        OH, OH                                           2880                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  Methyl   OH, OH                                           2881                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  Ethyl    OH, OH                                           2882                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl OH, OH                                           2883                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl  OH, OH                                           2884                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                      OH, OH                                           2885                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                           2886                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                           2887                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                           2888                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                           2889                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                           2890                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                             OH, OH                                           2891                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                           2892                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                           2893                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3 OH, OH                                           2894                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                       OH, OH                                           2895                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                           2896                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                           2897                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 -Ph                                                                             OH, OH                                           2898                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                     OH, OH                                           2899                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                           2900                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                           2901                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                     OH, OH                                           2902                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                           2903                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                           2904                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                       OH, OH                                           2905                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                           2906                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                           2907                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                             OH, OH                                           2908                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                     OH, OH                                           2909                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                     OH, OH                                           2910                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                           2911                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                           2912                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                           2913                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 -Ph                                                                          OH, OH                                           2914                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 -Ph                                                                          OH, OH                                           2915                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 H-Ph                                                                         OH, OH                                           2916                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 H-Ph                                                                         OH, OH                                           2917                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 H-Ph                                                                         OH, OH                                           2918                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 H-Ph                                                                         OH, OH                                           2919                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2920                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)-Ph                                                                       OH, OH                                           2921                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  H        (+)-pin                                          2922                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  Methyl   (+)-pin                                          2923                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  Ethyl    (+)-pin                                          2924                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl (+)-pin                                          2925                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl  (+)-pin                                          2926                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                      (+)-pin                                          2927                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                          2928                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                          2929                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                          2930                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                          2931                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                          2932                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                             (+)-pin                                          2933                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                          2934                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                          2935                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3 (+)-pin                                          2936                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                       (+)-pin                                          2937                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                          2938                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                          2939                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 -Ph                                                                             (+)-pin                                          2940                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                          2941                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                          2942                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                          2943                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                          2944                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                          2945                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                          2946                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                       (+)-pin                                          2947                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                          2948                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                          2949                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                             (+)-pin                                          2950                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                     (+)-pin                                          2951                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                     (+)-pin                                          2952                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                          2953                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                          2954                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                          2955                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 -Ph                                                                          (+)-pin                                          2956                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 -Ph                                                                          (+)-pin                                          2957                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 H-Ph                                                                         (+)-pin                                          2958                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 H-Ph                                                                         (+)-pin                                          2959                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 H-Ph                                                                         (+)-pin                                          2960                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 H-Ph                                                                         (+)-pin                                          2961                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2962                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          2963                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  H        OH, OH                                           2964                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  Methyl   OH, OH                                           2965                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  Ethyl    OH, OH                                           2966                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl OH, OH                                           2967                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl  OH, OH                                           2968                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                      OH, OH                                           2969                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                           2970                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                           2971                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                           2972                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                           2973                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                           2974                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                             OH, OH                                           2975                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                           2976                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                           2977                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3 OH, OH                                           2978                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                       OH, OH                                           2979                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                           2980                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                           2981                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 -Ph                                                                             OH, OH                                           2982                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                     OH, OH                                           2983                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                           2984                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                           2985                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                     OH, OH                                           2986                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                           2987                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                           2988                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                       OH, OH                                           2989                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                           2990                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                           2991                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                             OH, OH                                           2992                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                     OH, OH                                           2993                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                     OH, OH                                           2994                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                           2995                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                           2996                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                           2997                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 -Ph                                                                          OH, OH                                           2998                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 -Ph                                                                          OH, OH                                           2999                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 H-Ph                                                                         OH, OH                                           3000                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 H-Ph                                                                         OH, OH                                           3001                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 H-Ph                                                                         OH, OH                                           3002                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 H-Ph                                                                         OH, OH                                           3003                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)-Ph                                                                       OH, OH                                           3004                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)-Ph                                                                       OH, OH                                           3005                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  H        (+)-pin                                          3006                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  Methyl   (+)-pin                                          3007                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  Ethyl    (+)-pin                                          3008                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl (+)-pin                                          3009                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl  (+)-pin                                          3010                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                      (+)-pin                                          3011                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                          3012                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                          3013                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                          3014                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                          3015                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                          3016                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                             (+)-pin                                          3017                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                          3018                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                          3019                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3 (+)-pin                                          3020                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                       (+)-pin                                          3021                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                          3022                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                          3023                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 -Ph                                                                             (+)-pin                                          3024                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                          3025                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                          3026                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                          3027                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                          3028                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                          3029                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                          3030                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                       (+)-pin                                          3031                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                          3032                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                          3033                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                             (+)-pin                                          3034                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                     (+)-pin                                          3035                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                     (+)-pin                                          3036                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                          3037                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                          3038                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                          3039                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 -Ph                                                                          (+)-pin                                          3040                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 -Ph                                                                          (+)-pin                                          3041                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 H-Ph                                                                         (+)-pin                                          3042                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 H-Ph                                                                         (+)-pin                                          3043                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 H-Ph                                                                         (+)-pin                                          3044                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 H-Ph                                                                         (+)-pin                                          3045                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          3046                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          3047                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  H        OH, OH                                           3048                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  Methyl   OH, OH                                           3049                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  Ethyl    OH, OH                                           3050                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl OH, OH                                           3051                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl  OH, OH                                           3052                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                      OH, OH                                           3053                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                           3054                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                           3055                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                           3056                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                           3057                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                           3058                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                             OH, OH                                           3059                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                           3060                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                           3061                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3 OH, OH                                           3062                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                       OH, OH                                           3063                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                           3064                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                           3065                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 -Ph                                                                             OH, OH                                           3066                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                     OH, OH                                           3067                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                           3068                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                           3069                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                     OH, OH                                           3070                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                           3071                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                           3072                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                       OH, OH                                           3073                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                           3074                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                           3075                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                             OH, OH                                           3076                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                     OH, OH                                           3077                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                     OH, OH                                           3078                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                           3079                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                           3080                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                           3081                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 -Ph                                                                          OH, OH                                           3082                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 -Ph                                                                          OH, OH                                           3083                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 H-Ph                                                                         OH, OH                                           3084                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 H-Ph                                                                         OH, OH                                           3085                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 H-Ph                                                                         OH, OH                                           3086                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 H-Ph                                                                         OH, OH                                           3087                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)-Ph                                                                       OH, OH                                           3088                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)-Ph                                                                       OH, OH                                           3089                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    H        (+)-pin                                          3090                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    Methyl   (+)-pin                                          3091                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    Ethyl    (+)-pin                                          3092                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    n-Propyl (+)-pin                                          3093                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    n-Butyl  (+)-pin                                          3094                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 SCH.sub.3                                                                      (+)-pin                                          3095                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                          3096                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                          3097                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                          3098                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                          3099                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                          3100                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CN                                                                             (+)-pin                                          3101                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                          3102                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                          3103                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.3 (+)-pin                                          3104                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.3                                                                       (+)-pin                                          3105                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                          3106                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                          3107                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    F.sub.5 -Ph                                                                             (+)-pin                                          3108                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                          3109                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                          3110                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                          3111                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                          3112                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                          3113                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                          3114                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 NO.sub.2                                                                       (+)-pin                                          3115                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                          3116                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                          3117                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 OH                                                                             (+)-pin                                          3118                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 OH                                                                     (+)-pin                                          3119                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 OH                                                                     (+)-pin                                          3120                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                          3121                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                          3122                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                          3123                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-NO.sub.2 -Ph                                                                          (+)-pin                                          3124                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-NO.sub.2 -Ph                                                                          (+)-pin                                          3125                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-CO.sub.2 H-Ph                                                                         (+)-pin                                          3126                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-CO.sub.2 H-Ph                                                                         (+)-pin                                          3127                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-CN.sub.4 H-Ph                                                                         (+)-pin                                          3128                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-CN.sub.4 H-Ph                                                                         (+)-pin                                          3129                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          3130                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          3131                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    H        OH, OH                                           3132                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    Methyl   OH, OH                                           3133                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    Ethyl    OH, OH                                           3134                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    n-Propyl OH, OH                                           3135                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    n-Butyl  OH, OH                                           3136                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 SCH.sub.3                                                                      OH, OH                                           3137                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                           3138                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                           3139                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                           3140                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                           3141                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                           3142                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CN                                                                             OH, OH                                           3143                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                           3144                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                           3145                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.3 OH, OH                                           3146                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.3                                                                       OH, OH                                           3147                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                           3148                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                           3149                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    F.sub.5 -Ph                                                                             OH, OH                                           3150                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CO.sub.2 H                                                                     OH, OH                                           3151                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                           3152                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                           3153                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CN.sub.4 H                                                                     OH, OH                                           3154                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                           3155                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                           3156                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 NO.sub.2                                                                       OH, OH                                           3157                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                           3158                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                           3159                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 OH                                                                             OH, OH                                           3160                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 OH                                                                     OH, OH                                           3161                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 OH                                                                     OH, OH                                           3162                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                           3163                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                           3164                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                           3165                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-NO.sub.2 -Ph                                                                          OH, OH                                           3166                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-NO.sub.2 -Ph                                                                          OH, OH                                           3167                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-CO.sub.2 H-Ph                                                                         OH, OH                                           3168                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-CO.sub.2 H-Ph                                                                         OH, OH                                           3169                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-CN.sub.4 H-Ph                                                                         OH, OH                                           3170                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-CN.sub.4 H-Ph                                                                         OH, OH                                           3171                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-(HOCH.sub.2)-Ph                                                                       OH, OH                                           3172                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-(HOCH.sub.2)-Ph                                                                       OH, OH                                           3173                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           H        (+)-pin                                          3174                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           Methyl   (+)-pin                                          3175                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           Ethyl    (+)-pin                                          3176                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           n-Propyl (+)-pin                                          3177                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           n-Butyl  (+)-pin                                          3178                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                      (+)-pin                                          3179                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                          3180                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                          3181                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                          3182                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                          3183                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                          3184                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                             (+)-pin                                          3185                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                          3186                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                          3187                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.3 (+)-pin                                          3188                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                       (+)-pin                                          3189                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                          3190                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                          3191                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           F.sub.5 -Ph                                                                             (+)-pin                                          3192                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                          3193                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                          3194                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                          3195                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                          3196                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                          3197                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                          3198                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                       (+)-pin                                          3199                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                          3200                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                          3201                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                             (+)-pin                                          3202                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                     (+)-pin                                          3203                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                     (+)-pin                                          3204                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                          3205                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                          3206                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                          3207                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-NO.sub.2 -Ph                                                                          (+)-pin                                          3208                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-NO.sub.2 -Ph                                                                          (+)-pin                                          3209                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-CO.sub.2 H-Ph                                                                         (+)-pin                                          3210                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-CO.sub.2 H-Ph                                                                         (+)-pin                                          3211                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-CN.sub.4 H-Ph                                                                         (+)-pin                                          3212                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-CN.sub.4 H-Ph                                                                         (+)-pin                                          3213                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          3214                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          3215                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           H        OH, OH                                           3216                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           Methyl   OH, OH                                           3217                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           Ethyl    OH, OH                                           3218                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           n-Propyl OH, OH                                           3219                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           n-Butyl  OH, OH                                           3220                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                      OH, OH                                           3221                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                           3222                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                           3223                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                           3224                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                           3225                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                           3226                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                             OH, OH                                           3227                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                           3228                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                           3229                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.3 OH, OH                                           3230                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                       OH, OH                                           3231                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                           3232                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                           3233                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           F.sub.5 -Ph                                                                             OH, OH                                           3234                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                     OH, OH                                           3235                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                           3236                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                           3237                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                     OH, OH                                           3238                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                           3239                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                           3240                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                       OH, OH                                           3241                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                           3242                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                           3243                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                             OH, OH                                           3244                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                     OH, OH                                           3245                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                     OH, OH                                           3246                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                           3247                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                           3248                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                           3249                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-NO.sub.2 -Ph                                                                          OH, OH                                           3250                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-NO.sub.2 -Ph                                                                          OH, OH                                           3251                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-CO.sub.2 H-Ph                                                                         OH, OH                                           3252                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-CO.sub.2 H-Ph                                                                         OH, OH                                           3253                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-CN.sub.4 H-Ph                                                                         OH, OH                                           3254                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-CN.sub.4 H-Ph                                                                         OH, OH                                           3255                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-(HOCH.sub.2)-Ph                                                                       OH, OH                                           3256                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-(HOCH.sub.2)-Ph                                                                       OH, OH                                           3257                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  H        (+)-pin                                          3258                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  Methyl   (+)-pin                                          3259                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  Ethyl    (+)-pin                                          3260                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl (+)-pin                                          3261                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl  (+)-pin                                          3262                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                      (+)-pin                                          3263                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                   (+)-pin                                          3264                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                             (+)-pin                                          3265                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                             (+)-pin                                          3266                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          (+)-pin                                          3267                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   (+)-pin                                          3268                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                             (+)-pin                                          3269                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                    (+)-pin                                          3270                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           (+)-pin                                          3271                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3 (+)-pin                                          3272                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                       (+)-pin                                          3273                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                              (+)-pin                                          3274                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     (+)-pin                                          3275                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 -Ph                                                                             (+)-pin                                          3276                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                     (+)-pin                                          3277                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                             (+)-pin                                          3278                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                             (+)-pin                                          3279                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                     (+)-pin                                          3280                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                             (+)-pin                                          3281                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                             (+)-pin                                          3282                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                       (+)-pin                                          3283                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                               (+)-pin                                          3284                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                               (+)-pin                                          3285                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                             (+)-pin                                          3286                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                     (+)-pin                                          3287                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                     (+)-pin                                          3288                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                    (+)-pin                                          3289                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                            (+)-pin                                          3290                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                            (+)-pin                                          3291                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 -Ph                                                                          (+)-pin                                          3292                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 -Ph                                                                          (+)-pin                                          3293                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 H-Ph                                                                         (+)-pin                                          3294                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 H-Ph                                                                         (+)-pin                                          3295                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 H-Ph                                                                         (+)-pin                                          3296                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 H-Ph                                                                         (+)-pin                                          3297                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          3298                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)-Ph                                                                       (+)-pin                                          3299                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  H        OH, OH                                           3300                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  Methyl   OH, OH                                           3301                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  Ethyl    OH, OH                                           3302                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl OH, OH                                           3303                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl  OH, OH                                           3304                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                      OH, OH                                           3305                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                   OH, OH                                           3306                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                             OH, OH                                           3307                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                             OH, OH                                           3308                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                          OH, OH                                           3309                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                   OH, OH                                           3310                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                             OH, OH                                           3311                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                    OH, OH                                           3312                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                           OH, OH                                           3313                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3 OH, OH                                           3314                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                       OH, OH                                           3315                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                              OH, OH                                           3316                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                     OH, OH                                           3317                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 -Ph                                                                             OH, OH                                           3318                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                     OH, OH                                           3319                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                             OH, OH                                           3320                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                             OH, OH                                           3321                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                     OH, OH                                           3322                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                             OH, OH                                           3323                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                             OH, OH                                           3324                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                       OH, OH                                           3325                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                               OH, OH                                           3326                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                               OH, OH                                           3327                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                             OH, OH                                           3328                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                     OH, OH                                           3329                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                     OH, OH                                           3330                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                    OH, OH                                           3331                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                            OH, OH                                           3332                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                            OH, OH                                           3333                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 -Ph                                                                          OH, OH                                           3334                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 -Ph                                                                          OH, OH                                           3335                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 H-Ph                                                                         OH, OH                                           3336                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 H-Ph                                                                         OH, OH                                           3337                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 H-Ph                                                                         OH, OH                                           3338                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 H-Ph                                                                         OH, OH                                           3339                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)-Ph                                                                       OH, OH                                           3340                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)-Ph                                                                       OH, OH                                           __________________________________________________________________________      BA. MS (M+H).sup.+ : Calc. 480, Found 480.                                     BC. MS (M+H).sup.+ : Calc. 494, Found 494.                                     BD. MS (M+H).sup.+ : Calc. 522, Found 522.                                     BE. MS (M+H).sup.+ : Calc. 540, Found 540.                                     BF. MS (M+H).sup.+ : Calc. 519, Found 519.                                     BG. MS (M+H).sup.+ : Calc. 538, Found 538.                                     BH. MS (M+H).sup.+ : Calc. 346, Found 346.                                     BI. MS (M+H).sup.+ : Calc. 494, Found 494.                                     BJ. Anal. calcd. for C.sub.17 H.sub.26 BN.sub.5 O.sub.3.2H.sub.2 O.1.8HCl      C, 44.30; H, 6.95; Cl, 13.84; N, 15.20. Found: C, 44.22; H, 6.66; Cl,          14.03; N, 14.03.                                                               BW. MS (M+H).sup.+ : Calc. 466, Found 466.                                     BX. MS (M+H).sup.+ : Calc. 480, Found 480.                                     CV. MS (M+H).sup.+ : Calc. 510, Found 510.                                     CW. MS (M+H).sup.+ : Calc. 600, Found 600.                                     CX. MS (M+H).sup.+ : Calc. 552, Found 552.                                     CY. MS (M+H).sup.+ : Calc. 629, Found 629.                                     CZ. MS (M+H).sup.+ : Calc. 524, Found 524.                                     DA. MS (M+H).sup.+ : Calc. 614, Found 614.                               

                  TABLE 16                                                         ______________________________________                                          ##STR111##                                                                                                                Phys.                              Ex   X           m     R.sup.13                                                                              R.sup.14                                                                              Y.sup.1 Y.sup.2                                                                       Data                               ______________________________________                                         3345 CH.sub.2 NH.sub.2                                                                          1     Ph     Ph     (+)-pin                                   3346 CH.sub.2 NH.sub.2                                                                          1     Ph     PhCH.sub.2                                                                            (+)-pin                                   3347 CH.sub.2 NH.sub.2                                                                          1     Ph     Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3348 CH.sub.2 NH.sub.2                                                                          1     PhCH.sub.2                                                                            Ph     (+)-pin                                   3349 CH.sub.2 NH.sub.2                                                                          1     PhCH.sub.2                                                                            PhCH.sub.2                                                                            (+)-pin                                                                               BY                                 3350 CH.sub.2 NH.sub.2                                                                          1     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3351 CH.sub.2 NH.sub.2                                                                          1     Ph(CH.sub.2).sub.2                                                                    Ph     (+)-pin                                   3352 CH.sub.2 NH.sub.2                                                                          1     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            (+)-pin                                   3353 CH.sub.2 NH.sub.2                                                                          1     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3354 CH.sub.2 NH.sub.2                                                                          1     Ph     Ph     OH, OH                                    3355 CH.sub.2 NH.sub.2                                                                          1     Ph     PhCH.sub.2                                                                            OH, OH                                    3356 CH.sub.2 NH.sub.2                                                                          1     Ph     Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3357 CH.sub.2 NH.sub.2                                                                          1     PhCH.sub.2                                                                            Ph     OH, OH                                    3358 CH.sub.2 NH.sub.2                                                                          1     PhCH.sub.2                                                                            PhCH.sub.2                                                                            OH, OH                                    3359 CH.sub.2 NH.sub.2                                                                          1     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3360 CH.sub.2 NH.sub.2                                                                          1     Ph(CH.sub.2).sub.2                                                                    Ph     OH, OH                                    3361 CH.sub.2 NH.sub.2                                                                          1     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            OH, OH                                    3362 CH.sub.2 NH.sub.2                                                                          1     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3363 NH(CNH)NH.sub.2                                                                            1     Ph     Ph     (+)-pin                                   3364 NH(CNH)NH.sub.2                                                                            1     Ph     PhCH.sub.2                                                                            (+)-pin                                   3365 NH(CNH)NH.sub.2                                                                            1     Ph     Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3366 NH(CNH)NH.sub.2                                                                            1     PhCH.sub.2                                                                            Ph     (+)-pin                                   3367 NH(CNH)NH.sub.2                                                                            1     PhCH.sub.2                                                                            PhCH.sub.2                                                                            (+)-pin                                   3368 NH(CNH)NH.sub.2                                                                            1     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3369 NH(CNH)NH.sub.2                                                                            1     Ph(CH.sub.2).sub.2                                                                    Ph     (+)-pin                                   3370 NH(CNH)NH.sub.2                                                                            1     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            (+)-pin                                   3371 NH(CNH)NH.sub.2                                                                            1     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3372 NH(CNH)NH.sub.2                                                                            1     Ph     Ph     OH, OH                                    3373 NH(CNH)NH.sub.2                                                                            1     Ph     PhCH.sub.2                                                                            OH, OH                                    3374 NH(CNH)NH.sub.2                                                                            1     Ph     Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3375 NH(CNH)NH.sub.2                                                                            1     PhCH.sub.2                                                                            Ph     OH, OH                                    3376 NH(CNH)NH.sub.2                                                                            1     PhCH.sub.2                                                                            PhCH.sub.2                                                                            OH, OH                                    3377 NH(CNH)NH.sub.2                                                                            1     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3378 NH(CNH)NH.sub.2                                                                            1     Ph(CH.sub.2).sub.2                                                                    Ph     OH, OH                                    3379 NH(CNH)NH.sub.2                                                                            1     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            OH, OH                                    3380 NH(CNH)NH.sub.2                                                                            1     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3381 OMe         1     Ph     Ph     (+)-pin                                   3382 OMe         1     Ph     PhCH.sub.2                                                                            (+)-pin                                   3383 OMe         1     Ph     Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3384 OMe         1     PhCH.sub.2                                                                            Ph     (+)-pin                                   3385 OMe         1     PhCH.sub.2                                                                            PhCH.sub.2                                                                            (+)-pin                                   3386 OMe         1     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3387 OMe         1     Ph(CH.sub.2).sub.2                                                                    Ph     (+)-pin                                   3388 OMe         1     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            (+)-pin                                   3389 OMe         1     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3390 OMe         1     Ph     Ph     OH, OH                                    3391 OMe         1     Ph     PhCH.sub.2                                                                            OH, OH                                    3392 OMe         1     Ph     Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3393 OMe         1     PhCH.sub.2                                                                            Ph     OH, OH                                    3394 OMe         1     PhCH.sub.2                                                                            PhCH.sub.2                                                                            OH, OH                                    3395 OMe         1     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3396 OMe         1     Ph(CH.sub.2).sub.2                                                                    Ph     OH, OH                                    3397 OMe         1     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            OH, OH                                    3398 OMe         1     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3399 NH(CNH)H    1     Ph     Ph     (+)-pin                                   3400 NH(CNH)H    1     Ph     PhCH.sub.2                                                                            (+)-pin                                   3401 NH(CNH)H    1     Ph     Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3402 NH(CNH)H    1     PhCH.sub.2                                                                            Ph     (+)-pin                                   3403 NH(CNH)H    1     PhCH.sub.2                                                                            PhCH.sub.2                                                                            (+)-pin                                   3404 NH(CNH)H    1     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3405 NH(CNH)H    1     Ph(CH.sub.2).sub.2                                                                    Ph     (+)-pin                                   3406 NH(CNH)H    1     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            (+)-pin                                   3407 NH(CNH)H    1     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3408 NH(CNH)H    1     Ph     Ph     OH, OH                                    3409 NH(CNH)H    1     Ph     PhCH.sub.2                                                                            OH, OH                                    3410 NH(CNH)H    1     Ph     Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3411 NH(CNH)H    1     PhCH.sub.2                                                                            Ph     OH, OH                                    3412 NH(CNH)H    1     PhCH.sub.2                                                                            PhCH.sub.2                                                                            OH, OH                                    3413 NH(CNH)H    1     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3414 NH(CNH)H    1     Ph(CH.sub.2).sub.2                                                                    Ph     OH, OH                                    3415 NH(CNH)H    1     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            OH, OH                                    3416 NH(CNH)H    1     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3417 CH.sub.2 NH.sub.2                                                                          2     Ph     Ph     (+)-pin                                   3418 CH.sub.2 NH.sub.2                                                                          2     Ph     PhCH.sub.2                                                                            (+)-pin                                   3419 CH.sub.2 NH.sub.2                                                                          2     Ph     Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3420 CH.sub.2 NH.sub.2                                                                          2     PhCH.sub.2                                                                            Ph     (+)-pin                                   3421 CH.sub.2 NH.sub.2                                                                          2     PhCH.sub.2                                                                            PhCH.sub.2                                                                            (+)-pin                                   3422 CH.sub.2 NH.sub.2                                                                          2     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3423 CH.sub.2 NH.sub.2                                                                          2     Ph(CH.sub.2).sub.2                                                                    Ph     (+)-pin                                   3424 CH.sub.2 NH.sub.2                                                                          2     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            (+)-pin                                   3425 CH.sub.2 NH.sub.2                                                                          2     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3426 CH.sub.2 NH.sub.2                                                                          2     Ph     Ph     OH, OH                                    3427 CH.sub.2 NH.sub.2                                                                          2     Ph     PhCH.sub.2                                                                            OH, OH                                    3428 CH.sub.2 NH.sub.2                                                                          2     Ph     Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3429 CH.sub.2 NH.sub.2                                                                          2     PhCH.sub.2                                                                            Ph     OH, OH                                    3430 CH.sub.2 NH.sub.2                                                                          2     PhCH.sub.2                                                                            PhCH.sub.2                                                                            OH, OH                                    3431 CH.sub.2 NH.sub.2                                                                          2     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3432 CH.sub.2 NH.sub.2                                                                          2     Ph(CH.sub.2).sub.2                                                                    Ph     OH, OH                                    3433 CH.sub.2 NH.sub.2                                                                          2     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            OH, OH                                    3434 CH.sub.2 NH.sub.2                                                                          2     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3435 NH(CNH)NH.sub.2                                                                            2     Ph     Ph     (+)-pin                                   3436 NH(CNH)NH.sub.2                                                                            2     Ph     PhCH.sub.2                                                                            (+)-pin                                   3437 NH(CNH)NH.sub.2                                                                            2     Ph     Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3438 NH(CNH)NH.sub.2                                                                            2     PhCH.sub.2                                                                            Ph     (+)-pin                                   3439 NH(CNH)NH.sub.2                                                                            2     PhCH.sub.2                                                                            PhCH.sub.2                                                                            (+)-pin                                   3440 NH(CNH)NH.sub.2                                                                            2     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3441 NH(CNH)NH.sub.2                                                                            2     Ph(CH.sub.2).sub.2                                                                    Ph     (+)-pin                                   3442 NH(CNH)NH.sub.2                                                                            2     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            (+)-pin                                   3443 NH(CNH)NH.sub.2                                                                            2     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    (+)-pin                                   3444 NH(CNH)NH.sub.2                                                                            2     Ph     Ph     OH, OH                                    3445 NH(CNH)NH.sub.2                                                                            2     Ph     PhCH.sub.2                                                                            OH, OH                                    3446 NH(CNH)NH.sub.2                                                                            2     Ph     Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3447 NH(CNH)NH.sub.2                                                                            2     PhCH.sub.2                                                                            Ph     OH, OH                                    3448 NH(CNH)NH.sub.2                                                                            2     PhCH.sub.2                                                                            PhCH.sub.2                                                                            OH, OH                                    3449 NH(CNH)NH.sub.2                                                                            2     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    OH, OH                                    3450 NH(CNH)NH.sub.2                                                                            2     Ph(CH.sub.2).sub.2                                                                    Ph     OH, OH                                    3451 NH(CNH)NH.sub.2                                                                            2     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            OH, OH                                    3452 NH(CNH)NH.sub.2                                                                            2     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    OH, OH                                    ______________________________________                                          BY. MS (M+H).sup.+ : Calc. 570, Found 570.                               

                                      TABLE 17                                     __________________________________________________________________________      ##STR112##                                                                                                        Phys.                                      Ex X         R.sup.13                                                                            R.sup.14 R.sup.15                                                                           Y.sup.1 Y.sup.2                                                                     Data                                       __________________________________________________________________________     3457                                                                              CH.sub.2 NH.sub.2                                                                        Ph   H        H   (+)-pin                                         3458                                                                              CH.sub.2 NH.sub.2                                                                        Ph   methyl   H   (+)-pin                                                                             BK                                         3459                                                                              CH.sub.2 NH.sub.2                                                                        Ph   methyl   H   (+)-pin                                         3460                                                                              CH.sub.2 NH.sub.2                                                                        Ph   methyl   methyl                                                                             (+)-pin                                         3461                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    H   (+)-pin                                         3462                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    methyl                                                                             (+)-pin                                         3463                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    ethyl                                                                              (+)-pin                                         3464                                                                              CH.sub.2 NH.sub.2                                                                        Ph   isopropyl                                                                               H   (+)-pin                                         3465                                                                              CH.sub.2 NH.sub.2                                                                        Ph   phenyl   H   (+)-pin                                                                             BL                                         3466                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CN                                                                             H   (+)-pin                                         3467                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NC                                                                             H   (+)-pin                                         3468                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NO.sub.2                                                                       H   (+)-pin                                         3469                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SCH.sub.3                                                                      H   (+)-pin                                         3470                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SOCH.sub.3                                                                     H   (+)-pin                                         3471                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SO.sub.2 CH.sub.3                                                              H   (+)-pin                                         3472                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 OH                                                                             H   (+)-pin                                         3473                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 COOH                                                                           H   (+)-pin                                         3474                                                                              CH.sub.2 NH.sub.2                                                                        Ph   (CH.sub.2).sub.2 COOH                                                                   H   (+)-pin                                         3475                                                                              CH.sub.2 NH.sub.2                                                                        Ph   (CH.sub.2).sub.2 CN                                                                     H   (+)-pin                                         3476                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CHCHCOOMe                                                                               H   (+)-pin                                         3477                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CHCHCOOH H   (+)-pin                                         3478                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CHCHCN   H   (+)-pin                                         3479                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CN.sub.4 H                                                                     H   (+)-pin                                         3480                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NHSO.sub.2 CF.sub.3                                                            H   (+)-pin                                         3481                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 CN                                                                    H   (+)-pin                                         3482                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 NC                                                                    H   (+)-pin                                         3483                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 NO.sub.2                                                              H   (+)-pin                                         3484                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SCH.sub.3                                                             H   (+)-pin                                         3485                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SOCH.sub.3                                                            H   (+)-pin                                         3486                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                     H   (+)-pin                                         3487                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 CH.sub.2 OH                                                           H   (+)-pin                                         3488                                                                              CH.sub.2 NH.sub.2                                                                        Ph   NO.sub.2 H   (+)-pin                                         3489                                                                              CH.sub.2 NH.sub.2                                                                        Ph   F        H   (+)-pin                                         3490                                                                              CH.sub.2 NH.sub.2                                                                        Ph   OH       H   (+)-pin                                         3491                                                                              CH.sub.2 NH.sub.2                                                                        Ph   H        H   OH, OH                                          3492                                                                              CH.sub.2 NH.sub.2                                                                        Ph   methyl   H   OH, OH                                          3493                                                                              CH.sub.2 NH.sub.2                                                                        Ph   methyl   methyl                                                                             OH, OH                                          3494                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    H   OH, OH                                          3495                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    methyl                                                                             OH, OH                                          3496                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    ethyl                                                                              OH, OH                                          3497                                                                              CH.sub.2 NH.sub.2                                                                        Ph   isopropyl                                                                               H   OH, OH                                          3498                                                                              CH.sub.2 NH.sub.2                                                                        Ph   phenyl   H   OH, OH                                          3499                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CN                                                                             H   OH, OH                                          3500                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NC                                                                             H   OH, OH                                          3501                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NO.sub.2                                                                       H   OH, OH                                          3502                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SCH.sub.3                                                                      H   OH, OH                                          3503                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SOCH.sub.3                                                                     H   OH, OH                                          3504                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SO.sub.2 CH.sub.3                                                              H   OH, OH                                          3505                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 OH                                                                             H   OH, OH                                          3506                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 COOH                                                                           H   OH, OH                                          3507                                                                              CH.sub.2 NH.sub.2                                                                        Ph   (CH.sub.2).sub.2 COOH                                                                   H   OH, OH                                          3508                                                                              CH.sub.2 NH.sub.2                                                                        Ph   (CH.sub.2).sub.2 CN                                                                     H   OH, OH                                          3509                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CHCHCOOMe                                                                               H   OH, OH                                          3510                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CHCHCOOH H   OH, OH                                          3511                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CN.sub.4 H                                                                     H   OH, OH                                          3512                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NHSO.sub.2 CF.sub.3                                                            H   OH, OH                                          3513                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 CN                                                                    H   OH, OH                                          3514                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 NC                                                                    H   OH, OH                                          3515                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 NO.sub.2                                                              H   OH, OH                                          3516                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SCH.sub.3                                                             H   OH, OH                                          3517                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SOCH.sub.3                                                            H   OH, OH                                          3518                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                     H   OH, OH                                          3519                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 OH                                                                    H   OH, OH                                          3520                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 COOH                                                                  H   OH, OH                                          3521                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 CN.sub.4 H                                                            H   OH, OH                                          3522                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3                                                   H   OH, OH                                          3523                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H        H   (+)-pin                                         3524                                                                              CH.sub.2 NH.sub.2                                                                        PhO  methyl   H   (+)-pin                                         3525                                                                              CH.sub.2 NH.sub.2                                                                        PhS  methyl   methyl                                                                             (+)-pin                                         3526                                                                              CH.sub.2 NH.sub.2                                                                        PhNH ethyl    H   (+)-pin                                         3527                                                                              CH.sub.2 NH.sub.2                                                                        PhCONH                                                                              ethyl    methyl                                                                             (+)-pin                                         3528                                                                              CH.sub.2 NH.sub.2                                                                        PhNHCO                                                                              ethyl    ethyl                                                                              (+)-pin                                         3529                                                                              CH.sub.2 NH.sub.2                                                                        Ph   isopropyl                                                                               H   (+)-pin                                         3530                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          phenyl   H   (+)-pin                                         3531                                                                              CH.sub.2 NH.sub.2                                                                        PhO  CH.sub.2 CN                                                                             H   (+)-pin                                         3532                                                                              CH.sub.2 NH.sub.2                                                                        PhS  CH.sub.2 NC                                                                             H   (+)-pin                                         3533                                                                              CH.sub.2 NH.sub.2                                                                        PhNH CH.sub.2 NO.sub.2                                                                       H   (+)-pin                                         3534                                                                              CH.sub.2 NH.sub.2                                                                        PhCONH                                                                              CH.sub.2 SCH.sub.3                                                                      H   (+)-pin                                         3535                                                                              CH.sub.2 NH.sub.2                                                                        PhNHCO                                                                              CH.sub.2 SOCH.sub.3                                                                     H   (+)-pin                                         3536                                                                              CH.sub.2 NH.sub.2                                                                        Ph(CH.sub.2).sub.2                                                                  CH.sub.2 SO.sub.2 CH.sub.3                                                              H   (+)-pin                                         3537                                                                              NH(CNH)NH.sub.2                                                                          Ph   H        H   (+)-pin                                         3538                                                                              NH(CNH)NH.sub.2                                                                          Ph   methyl   H   (+)-pin                                                                             BM                                         3539                                                                              NH(CNH)NH.sub.2                                                                          Ph   methyl   H   (+)-pin                                         3540                                                                              NH(CNH)NH.sub.2                                                                          Ph   methyl   methyl                                                                             (+)-pin                                         3541                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    H   (+)-pin                                         3542                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    methyl                                                                             (+)-pin                                         3543                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    ethyl                                                                              (+)-pin                                         3544                                                                              NH(CNH)NH.sub.2                                                                          Ph   isopropyl                                                                               H   (+)-pin                                         3545                                                                              NH(CNH)NH.sub.2                                                                          Ph   phenyl   H   (+)-pin                                         3546                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CN                                                                             H   (+)-pin                                         3547                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NC                                                                             H   (+)-pin                                         3548                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NO.sub.2                                                                       H   (+)-pin                                         3549                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SCH.sub.3                                                                      H   (+)-pin                                         3550                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SOCH.sub.3                                                                     H   (+)-pin                                         3551                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SO.sub.2 CH.sub.3                                                              H   (+)-pin                                         3552                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 OH                                                                             H   (+)-pin                                         3553                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 COOH                                                                           H   (+)-pin                                         3554                                                                              NH(CNH)NH.sub.2                                                                          Ph   (CH.sub.2).sub.2 COOH                                                                   H   (+)-pin                                         3555                                                                              NH(CNH)NH.sub.2                                                                          Ph   (CH.sub.2).sub.2 CN                                                                     H   (+)-pin                                         3556                                                                              NH(CNH)NH.sub.2                                                                          Ph   CHCHCOOMe                                                                               H   (+)-pin                                         3557                                                                              NH(CNH)NH.sub.2                                                                          Ph   CHCHCOOH H   (+)-pin                                         3558                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CN.sub.4 H                                                                     H   (+)-pin                                         3559                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NHSO.sub.2 CF.sub.3                                                            H   (+)-pin                                         3560                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 CN                                                                    H   (+)-pin                                         3561                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 NC                                                                    H   (+)-pin                                         3562                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 NO.sub.2                                                              H   (+)-pin                                         3563                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SCH.sub.3                                                             H   (+)-pin                                         3564                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SOCH.sub.3                                                            H   (+)-pin                                         3565                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                     H   (+)-pin                                         3566                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 OH                                                                    H   (+)-pin                                         3567                                                                              NH(CNH)NH.sub.2                                                                          Ph   NO.sub.2 H   (+)-pin                                         3568                                                                              NH(CNH)NH.sub.2                                                                          Ph   F        H   (+)-pin                                         3569                                                                              NH(CNH)NH.sub.2                                                                          Ph   OH       H   (+)-pin                                         3570                                                                              NH(CNH)NH.sub.2                                                                          Ph   H        H   OH, OH                                          3571                                                                              NH(CNH)NH.sub.2                                                                          Ph   methyl   H   OH, OH                                          3572                                                                              NH(CNH)NH.sub.2                                                                          Ph   methyl   methyl                                                                             OH, OH                                          3573                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    H   OH, OH                                          3574                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    methyl                                                                             OH, OH                                          3575                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    ethyl                                                                              OH, OH                                          3576                                                                              NH(CNH)NH.sub.2                                                                          Ph   isopropyl                                                                               H   OH, OH                                          3577                                                                              NH(CNH)NH.sub.2                                                                          Ph   phenyl   H   OH, OH                                          3578                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CN                                                                             H   OH, OH                                          3579                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NC                                                                             H   OH, OH                                          3580                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NO.sub.2                                                                       H   OH, OH                                          3581                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SCH.sub.3                                                                      H   OH, OH                                          3582                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SOCH.sub.3                                                                     H   OH, OH                                          3583                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SO.sub.2 CH.sub.3                                                              H   OH, OH                                          3584                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 OH                                                                             H   OH, OH                                          3585                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 COOH                                                                           H   OH, OH                                          3586                                                                              NH(CNH)NH.sub.2                                                                          Ph   (CH.sub.2).sub.2 COOH                                                                   H   OH, OH                                          3587                                                                              NH(CNH)NH.sub.2                                                                          Ph   (CH.sub.2).sub.2 CN                                                                     H   OH, OH                                          3588                                                                              NH(CNH)NH.sub.2                                                                          Ph   CHCHCOOMe                                                                               H   OH, OH                                          3589                                                                              NH(CNH)NH.sub.2                                                                          Ph   CHCHCOOH H   OH, OH                                          3590                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CN.sub.4 H                                                                     H   OH, OH                                          3591                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NHSO.sub.2 CF.sub.3                                                            H   OH, OH                                          3592                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 CN                                                                    H   OH, OH                                          3593                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 NC                                                                    H   OH, OH                                          3594                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 NO.sub.2                                                              H   OH, OH                                          3595                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SCH.sub.3                                                             H   OH, OH                                          3596                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SOCH.sub.3                                                            H   OH, OH                                          3597                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                     H   OH, OH                                          3598                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 OH                                                                    H   OH, OH                                          3599                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 COOH                                                                  H   OH, OH                                          3600                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 CN.sub.4 H                                                            H   OH, OH                                          3601                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3                                                   H   OH, OH                                          3602                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H        H   (+)-pin                                         3603                                                                              NH(CNH)NH.sub.2                                                                          PhO  methyl   H   (+)-pin                                         3604                                                                              NH(CNH)NH.sub.2                                                                          PhS  methyl   methyl                                                                             (+)-pin                                         3605                                                                              NH(CNH)NH.sub.2                                                                          PhNH ethyl    H   (+)-pin                                         3606                                                                              NH(CNH)NH.sub.2                                                                          PhCONH                                                                              ethyl    methyl                                                                             (+)-pin                                         3607                                                                              NH(CNH)NH.sub.2                                                                          PhNHCO                                                                              ethyl    ethyl                                                                              (+)-pin                                         3608                                                                              NH(CNH)NH.sub.2                                                                          Ph   isopropyl                                                                               H   (+)-pin                                         3609                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          phenyl   H   (+)-pin                                         3610                                                                              NH(CNH)NH.sub.2                                                                          PhO  CH.sub.2 CN                                                                             H   (+)-pin                                         3611                                                                              NH(CNH)NH.sub.2                                                                          PhS  CH.sub.2 NC                                                                             H   (+)-pin                                         3612                                                                              NH(CNH)NH.sub.2                                                                          PhNH CH.sub.2 NO.sub.2                                                                       H   (+)-pin                                         3613                                                                              NH(CNH)NH.sub.2                                                                          PhCONH                                                                              CH.sub.2 SCH.sub.3                                                                      H   (+)-pin                                         3614                                                                              NH(CNH)NH.sub.2                                                                          PhNHCO                                                                              CH.sub.2 SOCH.sub.3                                                                     H   (+)-pin                                         3615                                                                              NH(CNH)NH.sub.2                                                                          Ph(CH.sub.2).sub.2                                                                  CH.sub.2 SO.sub.2 CH.sub.3                                                              H   (+)-pin                                         3616                                                                              OMe       Ph   CH.sub.3 H   (+)-pin                                         3617                                                                              NH(CNH)H  Ph   CH.sub.3 H   (+)-pin                                         3618                                                                              OMe       Ph   CH.sub.3 H   OH, OH                                          3619                                                                              NH(CNH)H  Ph   CH.sub.3 H   OH, OH                                          __________________________________________________________________________      BK. MS (M=H).sup.+ : Calc. 477, Found 477.                                     BL. MS (M=H).sup.+ : Calc. 539, Found 539.                                     BM. MS (M=H).sup.+ : Calc. 505, Found 505.                               

                                      TABLE 18                                     __________________________________________________________________________      ##STR113##                                                                                                        Phys.                                      Ex X         R.sup.13                                                                            R.sup.14 R.sup.15                                                                           Y.sup.1 Y.sup.2                                                                     Data                                       __________________________________________________________________________     3624                                                                              CH.sub.2 NH.sub.2                                                                        Ph   H        H   (+)-pin                                         3625                                                                              CH.sub.2 NH.sub.2                                                                        Ph   methyl   H   (+)-pin                                         3626                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    H   (+)-pin                                         3627                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    methyl                                                                             (+)-pin                                         3628                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    ethyl                                                                              (+)-pin                                         3629                                                                              CH.sub.2 NH.sub.2                                                                        Ph   isopropyl                                                                               H   (+)-pin                                         3630                                                                              CH.sub.2 NH.sub.2                                                                        Ph   phenyl   H   (+)-pin                                         3631                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CN                                                                             H   (+)-pin                                         3632                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NC                                                                             H   (+)-pin                                         3633                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NO.sub.2                                                                       H   (+)-pin                                         3634                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SCH.sub.3                                                                      H   (+)-pin                                         3635                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SOCH.sub.3                                                                     H   (+)-pin                                         3636                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SO.sub.2 CH.sub.3                                                              H   (+)-pin                                         3637                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 OH                                                                             H   (+)-pin                                         3638                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 COOH                                                                           H   (+)-pin                                         3639                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CN.sub.4 H                                                                     H   (+)-pin                                         3640                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NHSO.sub.2 CF.sub.3                                                            H   (+)-pin                                         3641                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 CN                                                                    H   (+)-pin                                         3642                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 NC                                                                    H   (+)-pin                                         3643                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 NO.sub.2                                                              H   (+)-pin                                         3644                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SCH.sub.3                                                             H   (+)-pin                                         3645                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SOCH.sub.3                                                            H   (+)-pin                                         3646                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                     H   (+)-pin                                         3647                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 CH.sub.2 OH                                                           H   (+)-pin                                         3648                                                                              CH.sub.2 NH.sub.2                                                                        Ph   NO.sub.2 H   (+)-pin                                         3649                                                                              CH.sub.2 NH.sub.2                                                                        Ph   F        H   (+)-pin                                         3650                                                                              CH.sub.2 NH.sub.2                                                                        Ph   OH       H   (+)-pin                                         3651                                                                              CH.sub.2 NH.sub.2                                                                        Ph   H        H   OH, OH                                          3652                                                                              CH.sub.2 NH.sub.2                                                                        Ph   methyl   H   OH, OH                                          3653                                                                              CH.sub.2 NH.sub.2                                                                        Ph   methyl   methyl                                                                             OH, OH                                          3654                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    H   OH, OH                                          3655                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    methyl                                                                             OH, OH                                          3656                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    ethyl                                                                              OH, OH                                          3657                                                                              CH.sub.2 NH.sub.2                                                                        Ph   isopropyl                                                                               H   OH, OH                                          3658                                                                              CH.sub.2 NH.sub.2                                                                        Ph   phenyl   H   OH, OH                                          3659                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CN                                                                             H   OH, OH                                          3660                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NC                                                                             H   OH, OH                                          3661                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NO.sub.2                                                                       H   OH, OH                                          3662                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SCH.sub.3                                                                      H   OH, OH                                          3663                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SOCH.sub.3                                                                     H   OH, OH                                          3664                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SO.sub.2 CH.sub.3                                                              H   OH, OH                                          3665                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 OH                                                                             H   OH, OH                                          3666                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 COOH                                                                           H   OH, OH                                          3667                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CN.sub.4 H                                                                     H   OH, OH                                          3668                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NHSO.sub.2 CF.sub.3                                                            H   OH, OH                                          3669                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 CN                                                                    H   OH, OH                                          3670                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 NC                                                                    H   OH, OH                                          3671                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 NO.sub.2                                                              H   OH, OH                                          3672                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SCH.sub.3                                                             H   OH, OH                                          3673                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SOCH.sub.3                                                            H   OH, OH                                          3674                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                     H   OH, OH                                          3675                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 OH                                                                    H   OH, OH                                          3676                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 COOH                                                                  H   OH, OH                                          3677                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 CN.sub.4 H                                                            H   OH, OH                                          3678                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3                                                   H   OH, OH                                          3679                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H        H   (+)-pin                                         3680                                                                              CH.sub.2 NH.sub.2                                                                        PhO  methyl   H   (+)-pin                                         3681                                                                              CH.sub.2 NH.sub.2                                                                        PhS  methyl   methyl                                                                             (+)-pin                                         3682                                                                              CH.sub.2 NH.sub.2                                                                        PhNH ethyl    H   (+)-pin                                         3683                                                                              CH.sub.2 NH.sub.2                                                                        PhCONH                                                                              ethyl    methyl                                                                             (+)-pin                                         3684                                                                              CH.sub.2 NH.sub.2                                                                        PhNHCO                                                                              ethyl    ethyl                                                                              (+)-pin                                         3685                                                                              CH.sub.2 NH.sub.2                                                                        Ph   isopropyl                                                                               H   (+)-pin                                         3686                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          phenyl   H   (+)-pin                                         3687                                                                              CH.sub.2 NH.sub.2                                                                        PhO  CH.sub.2 CN                                                                             H   (+)-pin                                         3688                                                                              CH.sub.2 NH.sub.2                                                                        PhS  CH.sub.2 NC                                                                             H   (+)-pin                                         3689                                                                              CH.sub.2 NH.sub.2                                                                        PhNH CH.sub.2 NO.sub.2                                                                       H   (+)-pin                                         3690                                                                              CH.sub.2 NH.sub.2                                                                        PhCONH                                                                              CH.sub.2 SCH.sub.3                                                                      H   (+)-pin                                         3691                                                                              CH.sub.2 NH.sub.2                                                                        PhNHCO                                                                              CH.sub.2 SOCH.sub.3                                                                     H   (+)-pin                                         3692                                                                              CH.sub.2 NH.sub.2                                                                        Ph(CH.sub.2).sub.2                                                                  CH.sub.2 SO.sub.2 CH.sub.3                                                              H   (+)-pin                                         3693                                                                              NH(CNH)NH.sub.2                                                                          Ph   H        H   (+)-pin                                         3694                                                                              NH(CNH)NH.sub.2                                                                          Ph   methyl   methyl                                                                             (+)-pin                                         3695                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    H   (+)-pin                                         3696                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    methyl                                                                             (+)-pin                                         3697                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    ethyl                                                                              (+)-pin                                         3698                                                                              NH(CNH)NH.sub.2                                                                          Ph   isopropyl                                                                               H   (+)-pin                                         3699                                                                              NH(CNH)NH.sub.2                                                                          Ph   phenyl   H   (+)-pin                                         3700                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CN                                                                             H   (+)-pin                                         3701                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NC                                                                             H   (+)-pin                                         3702                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NO.sub.2                                                                       H   (+)-pin                                         3703                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SCH.sub.3                                                                      H   (+)-pin                                         3704                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SOCH.sub.3                                                                     H   (+)-pin                                         3705                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SO.sub.2 CH.sub.3                                                              H   (+)-pin                                         3706                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 OH                                                                             H   (+)-pin                                         3707                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 COOH                                                                           H   (+)-pin                                         3708                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CN.sub.4 H                                                                     H   (+)-pin                                         3709                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NHSO.sub.2 CF.sub.3                                                            H   (+)-pin                                         3710                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 CN                                                                    H   (+)-pin                                         3711                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 NC                                                                    H   (+)-pin                                         3712                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 NO.sub.2                                                              H   (+)-pin                                         3713                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SCH.sub.3                                                             H   (+)-pin                                         3714                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SOCH.sub.3                                                            H   (+)-pin                                         3715                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                     H   (+)-pin                                         3716                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 OH                                                                    H   (+)-pin                                         3717                                                                              NH(CNH)NH.sub.2                                                                          Ph   NO.sub.2 H   (+)-pin                                         3718                                                                              NH(CNH)NH.sub.2                                                                          Ph   F        H   (+)-pin                                         3719                                                                              NH(CNH)NH.sub.2                                                                          Ph   OH       H   (+)-pin                                         3720                                                                              NH(CNH)NH.sub.2                                                                          Ph   H        H   OH, OH                                          3721                                                                              NH(CNH)NH.sub.2                                                                          Ph   methyl   H   OH, OH                                          3722                                                                              NH(CNH)NH.sub.2                                                                          Ph   methyl   methyl                                                                             OH, OH                                          3723                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    H   OH, OH                                          3724                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    methyl                                                                             OH, OH                                          3725                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    ethyl                                                                              OH, OH                                          3726                                                                              NH(CNH)NH.sub.2                                                                          Ph   isopropyl                                                                               H   OH, OH                                          3727                                                                              NH(CNH)NH.sub.2                                                                          Ph   phenyl   H   OH, OH                                          3728                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CN                                                                             H   OH, OH                                          3729                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NC                                                                             H   OH, OH                                          3730                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NO.sub.2                                                                       H   OH, OH                                          3731                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SCH.sub.3                                                                      H   OH, OH                                          3732                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SOCH.sub.3                                                                     H   OH, OH                                          3733                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SO.sub.2 CH.sub.3                                                              H   OH, OH                                          3734                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 OH                                                                             H   OH, OH                                          3735                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 COOH                                                                           H   OH, OH                                          3736                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CN.sub.4 H                                                                     H   OH, OH                                          3737                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NHSO.sub.2 CF.sub.3                                                            H   OH, OH                                          3738                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 CN                                                                    H   OH, OH                                          3739                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 NC                                                                    H   OH, OH                                          3740                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 NO.sub.2                                                              H   OH, OH                                          3741                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SCH.sub.3                                                             H   OH, OH                                          3742                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SOCH.sub.3                                                            H   OH, OH                                          3743                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                     H   OH, OH                                          3744                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 OH                                                                    H   OH, OH                                          3745                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 COOH                                                                  H   OH, OH                                          3746                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 CN.sub.4 H                                                            H   OH, OH                                          3747                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3                                                   H   OH, OH                                          3748                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H        H   (+)-pin                                         3749                                                                              NH(CNH)NH.sub.2                                                                          PhO  methyl   H   (+)-pin                                         3750                                                                              NH(CNH)NH.sub.2                                                                          PhS  methyl   methyl                                                                             (+)-pin                                         3751                                                                              NH(CNH)NH.sub.2                                                                          PhNH ethyl    H   (+)-pin                                         3752                                                                              NH(CNH)NH.sub.2                                                                          PhCONH                                                                              ethyl    methyl                                                                             (+)-pin                                         3753                                                                              NH(CNH)NH.sub.2                                                                          PhNHCO                                                                              ethyl    ethyl                                                                              (+)-pin                                         3754                                                                              NH(CNH)NH.sub.2                                                                          Ph   isopropyl                                                                               H   (+)-pin                                         3755                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          phenyl   H   (+)-pin                                         3756                                                                              NH(CNH)NH.sub.2                                                                          PhO  CH.sub.2 CN                                                                             H   (+)-pin                                         3757                                                                              NH(CNH)NH.sub.2                                                                          PhS  CH.sub.2 NC                                                                             H   (+)-pin                                         3758                                                                              NH(CNH)NH.sub.2                                                                          PhNH CH.sub.2 NO.sub.2                                                                       H   (+)-pin                                         3759                                                                              NH(CNH)NH.sub.2                                                                          PhCONH                                                                              CH.sub.2 SCH.sub.3                                                                      H   (+)-pin                                         3760                                                                              NH(CNH)NH.sub.2                                                                          PhNHCO                                                                              CH.sub.2 SOCH.sub.3                                                                     H   (+)-pin                                         3761                                                                              NH(CNH)NH.sub.2                                                                          Ph(CH.sub.2).sub.2                                                                  CH.sub.2 SO.sub.2 CH.sub.3                                                              H   (+)-pin                                         3762                                                                              OMe       Ph   CH.sub.3 H   (+)-pin                                         3763                                                                              NH(CNH)H  Ph   CH.sub.3 H   (+)-pin                                         3764                                                                              OMe       Ph   CH.sub.3 H   OH, OH                                          3765                                                                              NH(CNH)H  Ph   CH.sub.3 H   OH, OH                                          __________________________________________________________________________

                  TABLE 19                                                         ______________________________________                                          ##STR114##                                                                                                                Phys.                              Ex   X             R.sup.13                                                                              R.sup.14                                                                             R.sup.15                                                                            Y.sup.1 Y.sup.2                                                                       Data                               ______________________________________                                         3770 CH.sub.2 NH.sub.2                                                                            Ph     H     H    (+)-pin                                   3771 CH.sub.2 NH.sub.2                                                                            Ph     methyl                                                                               H    (+)-pin                                   3772 CH.sub.2 NH.sub.2                                                                            Ph     H     H    OH, OH                                    3773 CH.sub.2 NH.sub.2                                                                            Ph     methyl                                                                               H    OH, OH                                    3774 NH(CNH)NH.sub.2                                                                              Ph     H     H    (+)-pin                                   3775 NH(CNH)NH.sub.2                                                                              Ph     methyl                                                                               H    (+)-pin                                   3776 NH(CNH)NH.sub.2                                                                              Ph     H     H    OH, OH                                    3777 NH(CNH)NH.sub.2                                                                              Ph     methyl                                                                               H    OH, OH                                    3778 OMe           Ph     CH.sub.3                                                                             H    (+)-pin                                   3779 NH(CNH)H      Ph     CH.sub.3                                                                             H    (+)-pin                                   3780 OMe           Ph     CH.sub.3                                                                             H    OH, OH                                    3781 NH(CNH)H      Ph     CH.sub.3                                                                             H    OH, OH                                    ______________________________________                                    

                                      TABLE 20                                     __________________________________________________________________________      ##STR115##                                                                                                        Phys.                                      Ex X         R.sup.13                                                                            R.sup.14 R.sup.15                                                                           Y.sup.1 Y.sup.2                                                                     Data                                       __________________________________________________________________________     3786                                                                              CH.sub.2 NH.sub.2                                                                        Ph   H        H   (+)-pin                                         3787                                                                              CH.sub.2 NH.sub.2                                                                        Ph   methyl   methyl                                                                             (+)-pin                                         3788                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    H   (+)-pin                                         3789                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    methyl                                                                             (+)-pin                                         3790                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    ethyl                                                                              (+)-pin                                         3791                                                                              CH.sub.2 NH.sub.2                                                                        Ph   isopropyl                                                                               H   (+)-pin                                         3792                                                                              CH.sub.2 NH.sub.2                                                                        Ph   phenyl   H   (+)-pin                                         3793                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CN                                                                             H   (+)-pin                                         3794                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NC                                                                             H   (+)-pin                                         3795                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NO.sub.2                                                                       H   (+)-pin                                         3796                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SCH.sub.3                                                                      H   (+)-pin                                         3797                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SOCH.sub.3                                                                     H   (+)-pin                                         3798                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SO.sub.2 CH.sub.3                                                              H   (+)-pin                                         3799                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 OH                                                                             H   (+)-pin                                         3800                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 COOH                                                                           H   (+)-pin                                         3801                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CN.sub.4 H                                                                     H   (+)-pin                                         3802                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NHSO.sub.2 CF.sub.3                                                            H   (+)-pin                                         3803                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 CN                                                                    H   (+)-pin                                         3804                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 NC                                                                    H   (+)-pin                                         3805                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 NO.sub.2                                                              H   (+)-pin                                         3806                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SCH.sub.3                                                             H   (+)-pin                                         3807                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SOCH.sub.3                                                            H   (+)-pin                                         3808                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                     H   (+)-pin                                         3809                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 OH                                                                    H   (+)-pin                                         3810                                                                              CH.sub.2 NH.sub.2                                                                        Ph   NO.sub.2 H   (+)-pin                                         3811                                                                              CH.sub.2 NH.sub.2                                                                        Ph   F        H   (+)-pin                                         3812                                                                              CH.sub.2 NH.sub.2                                                                        Ph   OH       H   (+)-pin                                         3813                                                                              CH.sub.2 NH.sub.2                                                                        Ph   H        H   OH, OH                                          3814                                                                              CH.sub.2 NH.sub.2                                                                        Ph   methyl   H   OH, OH                                          3815                                                                              CH.sub.2 NH.sub.2                                                                        Ph   methyl   methyl                                                                             OH, OH                                          3816                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    H   OH, OH                                          3817                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    methyl                                                                             OH, OH                                          3818                                                                              CH.sub.2 NH.sub.2                                                                        Ph   ethyl    ethyl                                                                              OH, OH                                          3819                                                                              CH.sub.2 NH.sub.2                                                                        Ph   isopropyl                                                                               H   OH, OH                                          3820                                                                              CH.sub.2 NH.sub.2                                                                        Ph   phenyl   H   OH, OH                                          3821                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CN                                                                             H   OH, OH                                          3822                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NC                                                                             H   OH, OH                                          3823                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NO.sub.2                                                                       H   OH, OH                                          3824                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SCH.sub.3                                                                      H   OH, OH                                          3825                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SOCH.sub.3                                                                     H   OH, OH                                          3826                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 SO.sub.2 CH.sub.3                                                              H   OH, OH                                          3827                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 OH                                                                             H   OH, OH                                          3828                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 COOH                                                                           H   OH, OH                                          3829                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CN.sub.4 H                                                                     H   OH, OH                                          3830                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 NHSO.sub.2 CF.sub.3                                                            H   OH, OH                                          3831                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 CN                                                                    H   OH, OH                                          3832                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 NC                                                                    H   OH, OH                                          3833                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 NO.sub.2                                                              H   OH, OH                                          3834                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SCH.sub.3                                                             H   OH, OH                                          3835                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SOCH.sub.3                                                            H   OH, OH                                          3836                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                     H   OH, OH                                          3837                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 OH                                                                    H   OH, OH                                          3838                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 COOH                                                                  H   OH, OH                                          3839                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 CN.sub.4 H                                                            H   OH, OH                                          3840                                                                              CH.sub.2 NH.sub.2                                                                        Ph   CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3                                                   H   OH, OH                                          3841                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H        H   (+)-pin                                         3842                                                                              CH.sub.2 NH.sub.2                                                                        PhO  methyl   H   (+)-pin                                         3843                                                                              CH.sub.2 NH.sub.2                                                                        PhS  methyl   methyl                                                                             (+)-pin                                         3844                                                                              CH.sub.2 NH.sub.2                                                                        PhNH ethyl    H   (+)-pin                                         3845                                                                              CH.sub.2 NH.sub.2                                                                        PhCONH                                                                              ethyl    methyl                                                                             (+)-pin                                         3846                                                                              CH.sub.2 NH.sub.2                                                                        PhNHCO                                                                              ethyl    ethyl                                                                              (+)-pin                                         3847                                                                              CH.sub.2 NH.sub.2                                                                        Ph   isopropyl                                                                               H   (+)-pin                                         3848                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          phenyl   H   (+)-pin                                         3849                                                                              CH.sub.2 NH.sub.2                                                                        PhO  CH.sub.2 CN                                                                             H   (+)-pin                                         3850                                                                              CH.sub.2 NH.sub.2                                                                        PhS  CH.sub.2 NC                                                                             H   (+)-pin                                         3851                                                                              CH.sub.2 NH.sub.2                                                                        PhNH CH.sub.2 NO.sub.2                                                                       H   (+)-pin                                         3852                                                                              CH.sub.2 NH.sub.2                                                                        PhCONH                                                                              CH.sub.2 SCH.sub.3                                                                      H   (+)-pin                                         3853                                                                              CH.sub.2 NH.sub.2                                                                        PhNHCO                                                                              CH.sub.2 SOCH.sub.3                                                                     H   (+)-pin                                         3854                                                                              CH.sub.2 NH.sub.2                                                                        Ph(CH.sub.2).sub.2                                                                  CH.sub.2 SO.sub.2 CH.sub.3                                                              H   (+)-pin                                         3855                                                                              NH(CNH)NH.sub.2                                                                          Ph   H        H   (+)-pin                                         3856                                                                              NH(CNH)NH.sub.2                                                                          Ph   methyl   methyl                                                                             (+)-pin                                         3857                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    H   (+)-pin                                         3858                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    methyl                                                                             (+)-pin                                         3859                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    ethyl                                                                              (+)-pin                                         3860                                                                              NH(CNH)NH.sub.2                                                                          Ph   isopropyl                                                                               H   (+)-pin                                         3861                                                                              NH(CNH)NH.sub.2                                                                          Ph   phenyl   H   (+)-pin                                         3862                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CN                                                                             H   (+)-pin                                         3863                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NC                                                                             H   (+)-pin                                         3864                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NO.sub.2                                                                       H   (+)-pin                                         3865                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SCH.sub.3                                                                      H   (+)-pin                                         3866                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SOCH.sub.3                                                                     H   (+)-pin                                         3867                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SO.sub.2 CH.sub.3                                                              H   (+)-pin                                         3868                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 OH                                                                             H   (+)-pin                                         3869                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 COOH                                                                           H   (+)-pin                                         3870                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CN.sub.4 H                                                                     H   (+)-pin                                         3871                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NHSO.sub.2 CF.sub.3                                                            H   (+)-pin                                         3872                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 CN                                                                    H   (+)-pin                                         3873                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 NC                                                                    H   (+)-pin                                         3874                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 NO.sub.2                                                              H   (+)-pin                                         3875                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SCH.sub.3                                                             H   (+)-pin                                         3876                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SOCH.sub.3                                                            H   (+)-pin                                         3877                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                     H   (+)-pin                                         3878                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 OH                                                                    H   (+)-pin                                         3879                                                                              NH(CNH)NH.sub.2                                                                          Ph   NO.sub.2 H   (+)-pin                                         3880                                                                              NH(CNH)NH.sub.2                                                                          Ph   F        H   (+)-pin                                         3881                                                                              NH(CNH)NH.sub.2                                                                          Ph   OH       H   (+)-pin                                         3882                                                                              NH(CNH)NH.sub.2                                                                          Ph   H        H   OH, OH                                          3883                                                                              NH(CNH)NH.sub.2                                                                          Ph   methyl   H   OH, OH                                          3884                                                                              NH(CNH)NH.sub.2                                                                          Ph   methyl   methyl                                                                             OH, OH                                          3885                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    H   OH, OH                                          3886                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    methyl                                                                             OH, OH                                          3887                                                                              NH(CNH)NH.sub.2                                                                          Ph   ethyl    ethyl                                                                              OH, OH                                          3888                                                                              NH(CNH)NH.sub.2                                                                          Ph   isopropyl                                                                               H   OH, OH                                          3889                                                                              NH(CNH)NH.sub.2                                                                          Ph   phenyl   H   OH, OH                                          3890                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CN                                                                             H   OH, OH                                          3891                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NC                                                                             H   OH, OH                                          3892                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NO.sub.2                                                                       H   OH, OH                                          3893                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SCH.sub.3                                                                      H   OH, OH                                          3894                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SOCH.sub.3                                                                     H   OH, OH                                          3895                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 SO.sub.2 CH.sub.3                                                              H   OH, OH                                          3896                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 OH                                                                             H   OH, OH                                          3897                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 COOH                                                                           H   OH, OH                                          3898                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CN.sub.4 H                                                                     H   OH, OH                                          3899                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 NHSO.sub.2 CF.sub.3                                                            H   OH, OH                                          3900                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 CN                                                                    H   OH, OH                                          3901                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 NC                                                                    H   OH, OH                                          3902                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 NO.sub.2                                                              H   OH, OH                                          3903                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SCH.sub.3                                                             H   OH, OH                                          3904                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SOCH.sub.3                                                            H   OH, OH                                          3905                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                     H   OH, OH                                          3906                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 OH                                                                    H   OH, OH                                          3907                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 COOH                                                                  H   OH, OH                                          3908                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 CN.sub.4 H                                                            H   OH, OH                                          3909                                                                              NH(CNH)NH.sub.2                                                                          Ph   CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3                                                   H   OH, OH                                          3910                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H        H   (+)-pin                                         3911                                                                              NH(CNH)NH.sub.2                                                                          PhO  methyl   H   (+)-pin                                         3912                                                                              NH(CNH)NH.sub.2                                                                          PhS  methyl   methyl                                                                             (+)-pin                                         3913                                                                              NH(CNH)NH.sub.2                                                                          PhNH ethyl    H   (+)-pin                                         3914                                                                              NH(CNH)NH.sub.2                                                                          PhCONH                                                                              ethyl    methyl                                                                             (+)-pin                                         3915                                                                              NH(CNH)NH.sub.2                                                                          PhNHCO                                                                              ethyl    ethyl                                                                              (+)-pin                                         3916                                                                              NH(CNH)NH.sub.2                                                                          Ph   isopropyl                                                                               H   (+)-pin                                         3917                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          phenyl   H   (+)-pin                                         3918                                                                              NH(CNH)NH.sub.2                                                                          PhO  CH.sub.2 CN                                                                             H   (+)-pin                                         3919                                                                              NH(CNH)NH.sub.2                                                                          PhS  CH.sub.2 NC                                                                             H   (+)-pin                                         3920                                                                              NH(CNH)NH.sub.2                                                                          PhNH CH.sub.2 NO.sub.2                                                                       H   (+)-pin                                         3921                                                                              NH(CNH)NH.sub.2                                                                          PhCONH                                                                              CH.sub.2 SCH.sub.3                                                                      H   (+)-pin                                         3922                                                                              NH(CNH)NH.sub.2                                                                          PhNHCO                                                                              CH.sub.2 SOCH.sub.3                                                                     H   (+)-pin                                         3923                                                                              NH(CNH)NH.sub.2                                                                          Ph(CH.sub.2).sub.2                                                                  CH.sub.2 SO.sub.2 CH.sub.3                                                              H   (+)-pin                                         3924                                                                              OMe       Ph   CH.sub.3 H   (+)-pin                                         3925                                                                              NH(CNH)H  Ph   CH.sub.3 H   (+)-pin                                         3926                                                                              OMe       Ph   CH.sub.3 H   OH, OH                                          3927                                                                              NH(CNH)H  Ph   CH.sub.3 H   OH, OH                                          __________________________________________________________________________

                  TABLE 21                                                         ______________________________________                                          ##STR116##                                                                                                                Phys.                              Ex   X             R.sup.13                                                                              R.sup.14                                                                             R.sup.15                                                                            Y.sup.1 Y.sup.2                                                                       Data                               ______________________________________                                         3932 CH.sub.2 NH.sub.2                                                                            Ph     H     H    (+)-pin                                   3933 CH.sub.2 NH.sub.2                                                                            Ph     methyl                                                                               H    (+)-pin                                   3934 CH.sub.2 NH.sub.2                                                                            Ph     H     H    OH, OH                                    3935 CH.sub.2 NH.sub.2                                                                            Ph     methyl                                                                               H    OH, OH                                    3936 NH(CNH)NH.sub.2                                                                              Ph     H     H    (+)-pin                                   3937 NH(CNH)NH.sub.2                                                                              Ph     methyl                                                                               H    (+)-pin                                   3938 NH(CNH)NH.sub.2                                                                              Ph     H     H    OH, OH                                    3939 NH(CNH)NH.sub.2                                                                              Ph     methyl                                                                               H    OH, OH                                    3940 OMe           Ph     CH.sub.3                                                                             H    (+)-pin                                   3941 NH(CNH)H      Ph     CH.sub.3                                                                             H    (+)-pin                                   3942 OMe           Ph     CH.sub.3                                                                             H    OH, OH                                    3943 NH(CNH)H      Ph     CH.sub.3                                                                             H    OH, OH                                    ______________________________________                                    

                  TABLE 22                                                         ______________________________________                                          ##STR117##                                                                                                                Phys.                              Ex   X             R.sup.13                                                                              R.sup.14                                                                             R.sup.15                                                                            Y.sup.1 Y.sup.2                                                                       Data                               ______________________________________                                         3948 CH.sub.2 NH.sub.2                                                                            Ph     H     H    (+)-pin                                   3949 CH.sub.2 NH.sub.2                                                                            Ph     methyl                                                                               H    (+)-pin                                   3950 CH.sub.2 NH.sub.2                                                                            Ph     H     H    OH, OH                                    3951 CH.sub.2 NH.sub.2                                                                            Ph     methyl                                                                               H    OH, OH                                    3952 NH(CNH)NH.sub.2                                                                              Ph     H     H    (+)-pin                                   3953 NH(CNH)NH.sub.2                                                                              Ph     methyl                                                                               H    (+)-pin                                   3954 NH(CNH)NH.sub.2                                                                              Ph     H     H    OH, OH                                    3955 NH(CNH)NH.sub.2                                                                              Ph     methyl                                                                               H    OH, OH                                    3956 OMe           Ph     CH.sub.3                                                                             H    (+)-pin                                   3957 NH(CNH)H      Ph     CH.sub.3                                                                             H    (+)-pin                                   3958 OMe           Ph     CH.sub.3                                                                             H    OH, OH                                    3959 NH(CNH)H      Ph     CH.sub.3                                                                             H    OH, OH                                    ______________________________________                                    

                  TABLE 23                                                         ______________________________________                                          ##STR118##                                                                                                                Phys.                              Ex   X             R.sup.13                                                                              R.sup.14                                                                             R.sup.15                                                                            Y.sup.1 Y.sup.2                                                                       Data                               ______________________________________                                         3964 CH.sub.2 NH.sub.2                                                                            Ph     H     H    (+)-pin                                   3965 CH.sub.2 NH.sub.2                                                                            Ph     methyl                                                                               H    (+)-pin                                   3966 CH.sub.2 NH.sub.2                                                                            Ph     H     H    OH, OH                                    3967 CH.sub.2 NH.sub.2                                                                            Ph     methyl                                                                               H    OH, OH                                    3968 NH(CNH)NH.sub.2                                                                              Ph     H     H    (+)-pin                                   3969 NH(CNH)NH.sub.2                                                                              Ph     methyl                                                                               H    (+)-pin                                   3970 NH(CNH)NH.sub.2                                                                              Ph     H     H    OH, OH                                    3971 NH(CNH)NH.sub.2                                                                              Ph     methyl                                                                               H    OH, OH                                    3972 OMe           Ph     CH.sub.3                                                                             H    (+)-pin                                   3973 NH(CNH)H      Ph     CH.sub.3                                                                             H    (+)-pin                                   3974 OMe           Ph     CH.sub.3                                                                             H    OH, OH                                    3975 NH(CNH)H      Ph     CH.sub.3                                                                             H    OH, OH                                    ______________________________________                                    

                  TABLE 24                                                         ______________________________________                                          ##STR119##                                                                                                                Phys.                              Ex   X             R.sup.13                                                                              R.sup.14                                                                             R.sup.15                                                                            Y.sup.1 Y.sup.2                                                                       Data                               ______________________________________                                         3980 CH.sub.2 NH.sub.2                                                                            Ph     H     H    (+)-pin                                   3981 CH.sub.2 NH.sub.2                                                                            Ph     methyl                                                                               H    (+)-pin                                   3982 CH.sub.2 NH.sub.2                                                                            Ph     H     H    OH, OH                                    3983 CH.sub.2 NH.sub.2                                                                            Ph     methyl                                                                               H    OH, OH                                    3984 NH(CNH)NH.sub.2                                                                              Ph     H     H    (+)-pin                                   3985 NH(CNH)NH.sub.2                                                                              Ph     methyl                                                                               H    (+)-pin                                   3986 NH(CNH)NH.sub.2                                                                              Ph     H     H    OH, OH                                    3987 NH(CNH)NH.sub.2                                                                              Ph     methyl                                                                               H    OH, OH                                    3988 OMe           Ph     CH.sub.3                                                                             H    (+)-pin                                   3989 NH(CNH)H      Ph     CH.sub.3                                                                             H    (+)-pin                                   3990 OMe           Ph     CH.sub.3                                                                             H    OH, OH                                    3991 NH(CNH)H      Ph     CH.sub.3                                                                             H    OH, OH                                    ______________________________________                                    

                  TABLE 25                                                         ______________________________________                                          ##STR120##                                                                                                                Phys.                              Ex   X             R.sup.13                                                                              R.sup.14                                                                             R.sup.15                                                                            Y.sup.1 Y.sup.2                                                                       Data                               ______________________________________                                         3996 CH.sub.2 NH.sub.2                                                                            Ph     H     H    (+)-pin                                   3997 CH.sub.2 NH.sub.2                                                                            Ph     methyl                                                                               H    (+)-pin                                   3998 CH.sub.2 NH.sub.2                                                                            Ph     H     H    OH, OH                                    3999 CH.sub.2 NH.sub.2                                                                            Ph     methyl                                                                               H    OH, OH                                    4000 NH(CNH)NH.sub.2                                                                              Ph     H     H    (+)-pin                                   4001 NH(CNH)NH.sub.2                                                                              Ph     methyl                                                                               H    (+)-pin                                   4002 NH(CNH)NH.sub.2                                                                              Ph     H     H    OH, OH                                    4003 NH(CNH)NH.sub.2                                                                              Ph     methyl                                                                               H    OH, OH                                    4004 OMe           Ph     CH.sub.3                                                                             H    (+)-pin                                   4005 NH(CNH)H      Ph     CH.sub.3                                                                             H    (+)-pin                                   4006 OMe           Ph     CH.sub.3                                                                             H    OH, OH                                    4007 NH(CNH)H      Ph     CH.sub.3                                                                             H    OH, OH                                    ______________________________________                                    

                  TABLE 26                                                         ______________________________________                                          ##STR121##                                                                                                                Phys.                              Ex   X             R.sup.13                                                                              R.sup.14                                                                             R.sup.15                                                                            Y.sup.1 Y.sup.2                                                                       Data                               ______________________________________                                         4012 CH.sub.2 NH.sub.2                                                                            Ph     H     H    (+)-pin                                   4013 CH.sub.2 NH.sub.2                                                                            Ph     methyl                                                                               H    (+)-pin                                   4014 CH.sub.2 NH.sub.2                                                                            Ph     H     H    OH, OH                                    4015 CH.sub.2 NH.sub.2                                                                            Ph     methyl                                                                               H    OH, OH                                    4016 CH.sub.2 NH.sub.2                                                                            Ph     H     Ph   (+)-pin                                   4017 CH.sub.2 NH.sub.2                                                                            Ph     H     Ph   OH, OH                                    4018 NH(CNH)NH.sub.2                                                                              Ph     H     H    (+)-pin                                   4019 NH(CNH)NH.sub.2                                                                              Ph     methyl                                                                               H    (+)-pin                                   4020 NH(CNH)NH.sub.2                                                                              Ph     H     H    OH, OH                                    4021 NH(CNH)NH.sub.2                                                                              Ph     methyl                                                                               H    OH, OH                                    4022 NH(CNH)NH.sub.2                                                                              Ph     H     Ph   (+)-pin                                   4023 NH(CNH)NH.sub.2                                                                              Ph     H     Ph   OH, OH                                    4024 OMe           Ph     CH.sub.3                                                                             H    (+)-pin                                   4025 NH(CNH)H      Ph     CH.sub.3                                                                             H    (+)-pin                                   4026 OMe           Ph     CH.sub.3                                                                             H    OH, OH                                    4027 NH(CNH)H      Ph     CH.sub.3                                                                             H    OH, OH                                    ______________________________________                                    

                                      TABLE 27                                     __________________________________________________________________________      ##STR122##                                                                    Ex X        R.sup.13                                                                          R.sup.14                                                                            R.sup.15                                                                          R.sup.16                                                                           Y.sup.1 Y.sup.2                                                                     Phys. Data                                     __________________________________________________________________________     4032                                                                              CH.sub.2 NH.sub.2                                                                       Ph H    H  H   (+)-pin                                             4033                                                                              CH.sub.2 NH.sub.2                                                                       Ph methyl                                                                              H  H   (+)-pin                                             4034                                                                              CH.sub.2 NH.sub.2                                                                       Ph H    H  H   OH, OH                                              4035                                                                              CH.sub.2 NH.sub.2                                                                       Ph methyl                                                                              H  H   OH, OH                                              4036                                                                              NH(CNH)NH.sub.2                                                                         Ph H    H  H   (+)-pin                                             4037                                                                              NH(CNH)NH.sub.2                                                                         Ph methyl                                                                              H  H   (+)-pin                                             4038                                                                              NH(CNH)NH.sub.2                                                                         Ph H    H  H   OH, OH                                              4039                                                                              NH(CNH)NH.sub.2                                                                         Ph methyl                                                                              H  H   OH, OH                                              4040                                                                              NH(CNH)NH.sub.2                                                                         Ph H    CH.sub.3                                                                          CH.sub.3                                                                           (+)-pin                                             4041                                                                              NH(CNH)NH.sub.2                                                                         Ph H    CH.sub.3                                                                          CH.sub.3                                                                           OH, OH                                              4042                                                                              OMe      Ph CH.sub.3                                                                            H  H   (+)-pin                                             4043                                                                              NH(CNH)H Ph CH.sub.3                                                                            H  H   (+)-pin                                             4044                                                                              OMe      Ph CH.sub.3                                                                            H  H   OH, OH                                              4045                                                                              NH(CNH)H Ph CH.sub.3                                                                            H  H   OH, OH                                              __________________________________________________________________________

                                      TABLE 28                                     __________________________________________________________________________      ##STR123##                                                                    Ex X       R.sup.13                                                                          R.sup.14                                                                            R.sup.15                                                                          R.sup.16                                                                           Y.sup.1 Y.sup.2                                                                     Phys. Data                                      __________________________________________________________________________     4050                                                                              CH.sub.2 NH.sub.2                                                                      Ph CH.sub.2 CO.sub.2 H                                                                 H  H   (+)-pin                                              4051                                                                              CH.sub.2 NH.sub.2                                                                      Ph methyl                                                                              H  H   (+)-pin                                              4052                                                                              CH.sub.2 NH.sub.2                                                                      Ph CH.sub.2 CO.sub.2 H                                                                 H  H   OH, OH                                               4053                                                                              CH.sub.2 NH.sub.2                                                                      Ph methyl                                                                              H  H   OH, OH                                               4054                                                                              NH(CNH)NH.sub.2                                                                        Ph CH.sub.2 CN                                                                         H  H   (+)-pin                                              4055                                                                              NH(CNH)NH.sub.2                                                                        Ph methyl                                                                              H  H   (+)-pin                                              4056                                                                              NH(CNH)NH.sub.2                                                                        Ph CH.sub.2 CN                                                                         H  H   OH, OH                                               4057                                                                              NH(CNH)NH.sub.2                                                                        Ph methyl                                                                              H  H   OH, OH                                               4058                                                                              NH(CNH)NH.sub.2                                                                        Ph CH.sub.3                                                                            CH.sub.3                                                                          H   (+)-pin                                              4059                                                                              NH(CNH)NH.sub.2                                                                        Ph CH.sub.3                                                                            CH.sub.3                                                                          H   OH, OH                                               4060                                                                              OMe     Ph CH.sub.3                                                                            H  H   (+)-pin                                              4061                                                                              NH(CNH)H                                                                               Ph CH.sub.3                                                                            H  H   (+)-pin                                              4062                                                                              OMe     Ph CH.sub.3                                                                            H  H   OH, OH                                               4063                                                                              N(CNH)H Ph CH.sub.3                                                                            H  H   OH, OH                                               4064                                                                              CH.sub.2 NH.sub.2                                                                      Ph H    H  H   (+)-pin                                              4065                                                                              CH.sub.2 NH.sub.2                                                                      Ph H    H  H   OH, OH                                               __________________________________________________________________________

                                      TABLE 29                                     __________________________________________________________________________      ##STR124##                                                                    Ex X        R.sup.13                                                                          R.sup.14                                                                            R.sup.15                                                                          R.sup.16                                                                           Y.sup.1 Y.sup.2                                                                     Phys. Data                                     __________________________________________________________________________     4070                                                                              CH.sub.2 NH.sub.2                                                                       Ph H    H  H   (+)-pin                                             4071                                                                              CH.sub.2 NH.sub.2                                                                       Ph methyl                                                                              H  H   (+)-pin                                             4072                                                                              CH.sub.2 NH.sub.2                                                                       Ph H    H  H   OH, OH                                              4073                                                                              CH.sub.2 NH.sub.2                                                                       Ph methyl                                                                              H  H   OH, OH                                              4074                                                                              NH(CNH)NH.sub.2                                                                         Ph H    H  H   (+)-pin                                             4075                                                                              NH(CNH)NH.sub.2                                                                         Ph methyl                                                                              H  H   (+)-pin                                             4076                                                                              NH(CNH)NH.sub.2                                                                         Ph H    H  H   OH, OH                                              4077                                                                              NH(CNH)NH.sub.2                                                                         Ph methyl                                                                              H  H   OH, OH                                              4078                                                                              NH(CNH)NH.sub.2                                                                         Ph CH.sub.3                                                                            CH.sub.3                                                                          H   (+)-pin                                             4079                                                                              NH(CNH)NH.sub.2                                                                         Ph CH.sub.3                                                                            CH.sub.3                                                                          H   OH, OH                                              4080                                                                              OMe      Ph H    H  OH  (+)-pin                                             4081                                                                              NH(CNH)H Ph H    H  F   (+)-pin                                             4082                                                                              OMe      Ph H    H  Me  OH, OH                                              4083                                                                              NH(CNH)H Ph H    H  Et  OH, OH                                              __________________________________________________________________________

                                      TABLE 30                                     __________________________________________________________________________      ##STR125##                                                                                                     Phys.                                         Ex X       R.sup.13                                                                           R.sup.14                                                                          R.sup.15                                                                             R.sup.16                                                                           Y.sup.1 Y.sup.2                                                                     Data                                          __________________________________________________________________________     4088                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H  H     Cl  (+)-pin                                            4089                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H  methyl                                                                               H   (+)-pin                                            4090                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H  CH.sub.2 CN                                                                          H   (+)-pin                                            4091                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H  CH.sub.2 COOH                                                                        H   (+)-pin                                            4092                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H  CH.sub.2 NC                                                                          H   (+)-pin                                            4093                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H  CH.sub.2 NO.sub.2                                                                    H   (+)-pin                                            4094                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H  (CH.sub.2).sub.2 OH                                                                  H   (+)-pin                                            4095                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H  CH.sub.2 SOCH.sub.3                                                                  H   (+)-pin                                            4096                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H  H     NO.sub.2                                                                           OH, OH                                             4097                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H  methyl                                                                               H   OH, OH                                             4098                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H  CH.sub.2 CN                                                                          H   OH, OH                                             4099                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H  CH.sub.2 COOH                                                                        H   OH, OH                                             4100                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H  CH.sub.2 NC                                                                          H   OH, OH                                             4101                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H  CH.sub.2 NO.sub.2                                                                    H   OH, OH                                             4102                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H  (CH.sub.2).sub.2 OH                                                                  H   OH, OH                                             4103                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H  CH.sub.2 SOCH.sub.3                                                                  H   OH, OH                                             4104                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H  H     H   (+)-pin                                            4105                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H  methyl                                                                               H   (+)-pin                                            4106                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H  CH.sub.2 CN                                                                          H   (+)-pin                                            4107                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H  CH.sub.2 COOH                                                                        H   (+)-pin                                            4108                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H  CH.sub.2 NC                                                                          H   (+)-pin                                            4109                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H  CH.sub.2 NO.sub.2                                                                    H   (+)-pin                                            4110                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H  (CH.sub.2).sub.2 OH                                                                  H   (+)-pin                                            4111                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H  CH.sub.2 SOCH.sub.3                                                                  H   (+)-pin                                            4112                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H  H     H   OH, OH                                             4113                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H  methyl                                                                               H   OH, OH                                             4114                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H  CH.sub.2 CN                                                                          H   OH, OH                                             4115                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H  CH.sub.2 COOH                                                                        H   OH, OH                                             4116                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H  CH.sub.2 NC                                                                          H   OH, OH                                             4117                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H  CH.sub.2 NO.sub.2                                                                    H   OH, OH                                             4118                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H  (CH.sub.2).sub.2 OH                                                                  H   OH, OH                                             4119                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H  CH.sub.2 SOCH.sub.3                                                                  H   OH, OH                                             __________________________________________________________________________

                                      TABLE 31                                     __________________________________________________________________________      ##STR126##                                                                    Ex X       R.sup.13                                                                            R.sup.14                                                                          R.sup.15                                                                              Y.sup.1 Y.sup.2                                                                     Phys. Data                                      __________________________________________________________________________     4124                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  H      (+)-pin                                              4125                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  methyl (+)-pin                                              4126                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           (+)-pin                                              4127                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         (+)-pin                                              4128                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           (+)-pin                                              4129                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     (+)-pin                                              4130                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   (+)-pin                                              4131                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                              4132                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  H      OH, OH                                               4133                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  methyl OH, OH                                               4134                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           OH, OH                                               4135                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         OH, OH                                               4136                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           OH, OH                                               4137                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     OH, OH                                               4138                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   OH, OH                                               4139                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   OH, OH                                               4140                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  H      (+)-pin                                              4141                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  methyl (+)-pin                                              4142                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           (+)-pin                                              4143                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         (+)-pin                                              4144                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           (+)-pin                                              4145                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     (+)-pin                                              4146                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   (+)-pin                                              4147                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                              4148                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  H      OH, OH                                               4149                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  methyl OH, OH                                               4150                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           OH, OH                                               4151                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         OH, OH                                               4152                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           OH, OH                                               4153                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     OH, OH                                               4154                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   OH, OH                                               4155                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   OH, OH                                               __________________________________________________________________________

                                      TABLE 32                                     __________________________________________________________________________      ##STR127##                                                                    Ex X       R.sup.13                                                                            R.sup.14                                                                          R.sup.15                                                                              Y.sup.1 Y.sup.2                                                                     Phys. Data                                      __________________________________________________________________________     4160                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  H      (+)-pin                                              4161                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          Cl H      (+)-pin                                              4162                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  methyl (+)-pin                                              4163                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           (+)-pin                                              4164                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          Cl CH.sub.2 CN                                                                           (+)-pin                                              4165                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         (+)-pin                                              4166                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           (+)-pin                                              4167                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     (+)-pin                                              4168                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   (+)-pin                                              4169                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                              4170                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  H      OH, OH                                               4171                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          Cl H      OH, OH                                               4172                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  methyl OH, OH                                               4173                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           OH, OH                                               4174                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          Cl CH.sub.2 CN                                                                           OH, OH                                               4175                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         OH, OH                                               4176                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           OH, OH                                               4177                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     OH, OH                                               4178                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   OH, OH                                               4179                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   OH, OH                                               4180                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  H      (+)-pin                                              4181                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  methyl (+)-pin                                              4182                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           (+)-pin                                              4183                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         (+)-pin                                              4184                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           (+)-pin                                              4185                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     (+)-pin                                              4186                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   (+)-pin                                              4187                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                              4188                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  H      OH, OH                                               4189                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  methyl OH, OH                                               4190                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           OH, OH                                               4191                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         OH, OH                                               4192                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           OH, OH                                               4193                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     OH, OH                                               4194                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   OH, OH                                               4195                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   OH, OH                                               __________________________________________________________________________

                  TABLE 33                                                         ______________________________________                                          ##STR128##                                                                                                             Phys.                                 Ex   X           R.sup.13                                                                               R.sup.14 Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         4200 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4201 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4202 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4203 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4204 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4205 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4206 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4207 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4208 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4209 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4210 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4211 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4212 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4213 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4214 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4215 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4216 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4217 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4218 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4219 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4220 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4221 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4222 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4223 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                 4224 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4225 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4226 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4227 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4228 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       4229 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4230 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4231 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4232 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4233 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4234 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4235 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4236 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4237 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       ______________________________________                                    

                  TABLE 34                                                         ______________________________________                                          ##STR129##                                                                    Ex    X            R.sup.13   Y.sup.1 Y.sup.2                                                                        Phys. Data                               ______________________________________                                         m = 1                                                                          4242  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 (+)-pin                                          4243  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 OH, OH                                           4244  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 (+)-pin                                          4245  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 OH, OH                                           4246  OMe          PhCH.sub.2 (+)-pin                                          4247  OMe          PhCH.sub.2 OH, OH                                           4248  NH(CNH)H     PhCH.sub.2 (+)-pin                                          4249  NH(CNH)H     PhCH.sub.2 OH, OH                                           4250  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       (+)-pin DB                                       4251  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           4252  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          4253  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           4254  OMe          PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          4255  OMe          PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           4256  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          4257  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       OH, OH  DC                                       4258  CH.sub.2 NH.sub.2                                                                           Ph         (+)-pin                                          4259  CH.sub.2 NH.sub.2                                                                           Ph         OH, OH                                           4260  NH(CNH)NH.sub.2                                                                             Ph         (+)-pin                                          4261  NH(CNH)NH.sub.2                                                                             Ph         OH, OH                                           4262  OMe          Ph         (+)-pin                                          4263  OMe          Ph         OH, OH                                           4264  NH(CNH)H     Ph         (+)-pin                                          4265  NH(CNH)H     Ph         OH, OH                                           4266  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2 S                                                                     (+)-pin                                          4267  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 S                                                                              (+)-pin                                          4268  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2 S                                                                     OH, OH                                           4269  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 S                                                                              OH, OH                                           4270  m = 2                                                                    4271  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 (+)-pin                                          4272  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 OH, OH                                           4273  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 (+)-pin                                          4274  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 OH, OH                                           4275  OMe          PhCH.sub.2 (+)-pin                                          4276  OMe          PhCH.sub.2 OH, OH                                           4277  NH(CNH)H     PhCH.sub.2 (+)-pin                                          4278  NH(CNH)H     PhCH.sub.2 OH, OH                                           4279  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          4280  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           4281  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          4282  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           4283  OMe          PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          4284  OMe          PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           4285  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          4286  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           4287  CH.sub.2 NH.sub.2                                                                           Ph         (+)-pin                                          4288  CH.sub.2 NH.sub.2                                                                           Ph         OH, OH                                           4289  NH(CNH)NH.sub.2                                                                             Ph         (+)-pin                                          4290  NH(CNH)NH.sub.2                                                                             Ph         OH, OH                                           4291  OMe          Ph         (+)-pin                                          4292  OMe          Ph         OH, OH                                           4293  NH(CNH)H     Ph         (+)-pin                                          4294  NH(CNH)H     Ph         OH, OH                                           ______________________________________                                          DB. HRMS Calc'd. 495.3255, Found 495.3257                                      DC. HRMS Calc'd. 467.2442, Found 467.2950                                

                  TABLE 35                                                         ______________________________________                                          ##STR130##                                                                    Ex    X            R.sup.13   Y.sup.1 Y.sup.2                                                                        Phys. Data                               ______________________________________                                         m = 1                                                                          4299  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 (+)-pin                                          4300  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 OH, OH                                           4301  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 (+)-pin                                          4302  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 OH, OH                                           4303  OMe          PhCH.sub.2 (+)-pin                                          4304  OMe          PhCH.sub.2 OH, OH                                           4305  NH(CNH)H     PhCH.sub.2 (+)-pin                                          4306  NH(CNH)H     PhCH.sub.2 OH, OH                                           4307  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       (+)-pin DE                                       4308  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           4309  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          4310  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           4311  OMe          PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          4312  OMe          PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           4313  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          4314  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           4315  CH.sub.2 NH.sub.2                                                                           Ph         (+)-pin                                          4316  CH.sub.2 NH.sub.2                                                                           Ph         OH, OH                                           4317  NH(CNH)NH.sub.2                                                                             Ph         (+)-pin                                          4318  NH(CNH)NH.sub.2                                                                             Ph         OH, OH                                           4319  OMe          Ph         (+)-pin                                          4320  OMe          Ph         OH, OH                                           4321  NH(CNH)H     Ph         (+)-pin                                          4322  NH(CNH)H     Ph         OH, OH                                           4323  m = 2                                                                    4324  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 (+)-pin                                          4325  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 OH, OH                                           4326  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 (+)-pin                                          4327  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 OH, OH                                           4328  OMe          PhCH.sub.2 (+)-pin                                          4329  OMe          PhCH.sub.2 OH, OH                                           4330  NH(CNH)H     PhCH.sub.2 (+)-pin                                          4331  NH(CNH)H     PhCH.sub.2 OH, OH                                           4332  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          4333  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           4334  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          4335  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           4336  OMe          PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          4337  OMe          PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           4338  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          4339  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           4340  CH.sub.2 NH.sub.2                                                                           Ph         (+)-pin                                          4341  CH.sub.2 NH.sub.2                                                                           Ph         OH, OH                                           4342  NH(CNH)NH.sub.2                                                                             Ph         (+)-pin                                          4343  NH(CNH)NH.sub.2                                                                             Ph         OH, OH                                           4344  OMe          Ph         (+)-pin                                          4345  OMe          Ph         OH, OH                                           4346  NH(CNH)H     Ph         (+)-pin                                          4347  NH(CNH)H     Ph         OH, OH                                           ______________________________________                                          DE. HRMS Calc'd. 495.3255, Found 495.3249                                

                  TABLE 36                                                         ______________________________________                                          ##STR131##                                                                                                             Phys.                                 Ex   X           R.sup.13                                                                               R.sup.14 Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         m = 1                                                                          4348 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4349 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4350 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4351 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4352 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4353 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4354 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4355 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4356 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4357 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4358 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4359 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4360 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4361 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4362 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4363 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4364 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4365 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4366 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4367 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4368 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4369 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4370 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4371 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4372 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4373 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4374 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        H, OH                                        4375 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4376 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4377 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4378 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4379 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4380 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4381 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4382 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4383 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4384 m = 2                                                                     4385 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4386 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4387 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4388 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4389 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4390 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4391 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4392 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4393 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4394 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4395 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4396 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4397 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4398 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4399 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4400 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4401 NH(CNH)NH.sub.2                                                                            PhCH.sub.2       (+)-pin                                      4402 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             ethyl    (+)-pin                                      4403 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4404 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4405 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4406 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4407 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4408 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4409 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4410 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4411 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       4412 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4413 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4414 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4415 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4416 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4417 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4418 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4419 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4420 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4421 m = 0                                                                     4422 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4423 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4424 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4425 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4426 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4427 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4428 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4429 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4430 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4431 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4432 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4433 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4434 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4435 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4436 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4437 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4438 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4439 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4440 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4441 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4442 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4443 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4444 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4445 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4446 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4447 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4448 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        H, OH                                        4449 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4450 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4451 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4452 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4453 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4454 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4455 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4456 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4457 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       ______________________________________                                    

                  TABLE 37                                                         ______________________________________                                          ##STR132##                                                                                                             Phys.                                 Ex   X           R.sup.13                                                                               R.sup.14 Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         m = 1                                                                          4462 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4463 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4464 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4465 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4466 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4467 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4468 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4469 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4470 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4471 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4472 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4473 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4474 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4475 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4476 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4477 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4478 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4479 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4480 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4481 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4482 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4483 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4484 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4485 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4486 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4487 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4488 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       4489 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4490 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4491 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4492 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4493 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4494 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4495 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4496 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4497 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4498 m = 2                                                                     4499 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4500 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4501 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4502 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4503 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4504 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4505 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4506 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4507 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4508 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4509 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4510 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4511 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4512 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4513 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4514 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4515 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4516 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4517 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4518 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4519 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4520 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4521 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4522 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4523 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4524 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4525 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       4526 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4527 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4528 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4529 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4530 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4531 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4532 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4533 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4534 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                            m = 0                                                                     4535 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4536 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4537 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4538 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4539 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4540 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4541 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4542 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4543 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4544 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4545 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4546 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4547 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4548 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4549 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4550 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4551 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4552 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4553 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4554 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4555 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4556 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4557 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4558 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4559 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4560 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4561 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       4562 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4563 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4564 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4565 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4566 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4567 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4568 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4569 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4570 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       ______________________________________                                    

                  TABLE 38                                                         ______________________________________                                          ##STR133##                                                                                                             Phys.                                 Ex   X           R.sup.13                                                                               R.sup.14 Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         m = 1                                                                          4575 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4576 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4577 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4578 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4579 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4580 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4581 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4582 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4583 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4584 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4585 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4586 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4587 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4588 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4589 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4590 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4591 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4592 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4593 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4594 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4595 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4596 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4597 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4598 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4599 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4600 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4601 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       4602 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4603 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4604 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4605 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4606 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4607 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4608 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4609 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4610 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                            m = 0                                                                     4611 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4612 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4613 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4614 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4615 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4616 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4617 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4618 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4619 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4620 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4621 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4622 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4623 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4624 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4625 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4626 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4627 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4628 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4629 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4630 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4631 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4632 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4633 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4634 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4635 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4636 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4637 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       4638 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4639 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4640 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4641 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4642 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4643 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4644 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4645 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4646 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       ______________________________________                                    

                  TABLE 39                                                         ______________________________________                                          ##STR134##                                                                                                             Phys.                                 Ex   X           R.sup.13                                                                               R.sup.14 Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         m = 1                                                                          4651 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4652 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4653 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4654 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4655 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4656 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4657 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4658 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4659 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4660 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4661 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4662 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4663 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4664 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4665 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4666 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4667 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4668 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4669 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4670 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4671 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4672 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4673 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4674 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4675 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4676 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4677 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       4678 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4679 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4680 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4681 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4682 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4683 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4684 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4685 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4686 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                            m = 0                                                                     4687 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4688 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4689 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4690 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4691 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4692 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4693 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4694 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4695 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4696 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4697 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4698 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4699 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4700 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4701 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4702 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4703 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4704 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4705 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4706 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4707 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4708 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4709 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4710 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4711 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4712 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4713 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       4714 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4715 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4716 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4717 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4718 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4719 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4720 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4721 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4722 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       ______________________________________                                    

                  TABLE 40                                                         ______________________________________                                          ##STR135##                                                                                                             Phys.                                 Ex   X           R.sup.13                                                                               R.sup.14 Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         m = 1                                                                          4727 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4728 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4729 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4730 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4731 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4732 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4733 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4734 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4735 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4736 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4737 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4738 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4739 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4740 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4741 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4742 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4743 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4744 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4745 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4746 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4747 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4748 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4749 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4750 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4751 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4752 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4753 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       4754 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4755 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4756 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4757 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4758 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4759 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4760 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4761 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4762 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                            m = 0                                                                     4763 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4764 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4765 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4766 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4767 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4768 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4769 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4770 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4771 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4772 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4773 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4774 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4775 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4776 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4777 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4778 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4779 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4780 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4781 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4782 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4783 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4784 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4785 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4786 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4787 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4788 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4789 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       4790 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4791 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4792 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4793 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4794 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4795 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4796 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4797 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4798 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       ______________________________________                                    

                  TABLE 41                                                         ______________________________________                                          ##STR136##                                                                                                             Phys.                                 Ex   X           R.sup.13                                                                               R.sup.14 Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         m = 1                                                                          4803 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4804 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4805 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4806 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4807 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4808 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4809 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4810 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4811 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4812 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4813 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4814 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4815 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4816 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4817 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4818 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4819 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4820 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4821 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4822 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4823 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4824 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4825 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4826 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4827 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4828 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4829 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       4830 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4831 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4832 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4833 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4834 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4835 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4836 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4837 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4838 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                            m = 0                                                                     4839 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4840 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4841 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4842 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4843 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4844 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4845 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4846 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4847 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4848 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4849 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4850 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4851 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4852 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4853 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4854 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4855 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4856 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4857 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4858 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4859 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4860 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4861 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4862 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4863 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4864 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4865 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       4866 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4867 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4868 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4869 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4870 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4871 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4872 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4873 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4874 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       ______________________________________                                    

                  TABLE 42                                                         ______________________________________                                          ##STR137##                                                                                                             Phys.                                 Ex   X           R.sup.13                                                                               R.sup.14 Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         m = 1                                                                          4879 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4880 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4881 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4882 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4883 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4884 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4885 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4886 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4887 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4888 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4889 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4890 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4891 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4892 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4893 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4894 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4895 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4896 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4897 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4898 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4899 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4900 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4901 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4902 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4903 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4904 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4905 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       4906 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4907 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4908 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4909 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4910 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4911 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4912 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4913 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4914 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                            m = 2                                                                     4915 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4916 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4917 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4918 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4919 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4920 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4921 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4922 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4923 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4924 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4925 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4926 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4927 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4928 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4929 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4930 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4931 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4932 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4933 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4934 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4935 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4936 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4937 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4938 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4939 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4940 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4941 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       4942 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4943 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4944 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4945 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4946 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4947 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4948 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4949 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4950 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                            m = 0                                                                     4951 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4952 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4953 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4954 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4955 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4956 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4957 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4958 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4959 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       4960 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       4961 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4962 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4963 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4964 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4965 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4966 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       4967 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      4968 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      4969 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4970 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      4971 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4972 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      4973 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4974 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4975 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4976 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4977 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       4978 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       4979 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       4980 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       4981 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       4982 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       4983 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       4984 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       4985 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       4986 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       ______________________________________                                    

                  TABLE 43                                                         ______________________________________                                          ##STR138##                                                                                                             Phys.                                 Ex   X           R.sup.13                                                                               R.sup.14 Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         m = 1                                                                          4991 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      4992 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      4993 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      4994 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      4995 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      4996 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      4997 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      4998 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      4999 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       5000 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       5001 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       5002 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       5003 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       5004 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       5005 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       5006 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       5007 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      5008 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      5009 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      5010 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      5011 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      5012 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      5013 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      5014 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      5015 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      5016 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      5017 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       5018 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       5019 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       5020 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       5021 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       5022 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       5023 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       5024 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       5025 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       5026 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                            m = 2                                                                     5027 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      5028 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      5029 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      5030 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      5031 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      5032 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      5033 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      5034 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      5035 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       5036 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       5037 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       5038 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       5039 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       5040 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       5041 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       5042 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       5043 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      5044 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      5045 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      5046 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      5047 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      5048 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      5049 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      5050 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      5051 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      5052 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      5053 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       5054 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       5055 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       5056 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       5057 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       5058 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       5059 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       5060 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       5061 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       5062 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                            m = 0                                                                     5063 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      5064 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      5065 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      5066 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      5067 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      5068 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      5069 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      5070 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      5071 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       5072 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       5073 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       5074 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       5075 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       5076 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       5077 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       5078 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       5079 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      5080 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      5081 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      5082 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      5083 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      5084 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      5085 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      5086 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      5087 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      5088 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      5089 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       5090 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       5091 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       5092 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       5093 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       5094 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       5095 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       5096 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       5097 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       5098 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       ______________________________________                                    

                  TABLE 44                                                         ______________________________________                                          ##STR139##                                                                                                             Phys.                                 Ex   X           R.sup.13                                                                               R.sup.14 Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         m = 1                                                                          5103 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      5104 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      5105 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      5106 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      5107 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      5108 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      5109 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      5110 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      5111 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       5112 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       5113 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       5114 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       5115 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       5116 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       5117 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       5118 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       5119 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      5120 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      5121 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      5122 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      5123 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      5124 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      5125 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      5126 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      5127 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      5128 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      5129 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       5130 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       5131 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       5132 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       5133 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       5134 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       5135 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       5136 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       5137 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       5138 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                            m = 2                                                                     5139 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      5140 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      5141 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      5142 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      5143 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      5144 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      5145 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      5146 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      5147 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       5148 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       5149 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       5150 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       5151 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       5152 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       5153 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       5154 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       5155 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      5156 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      5157 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      5158 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      5159 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      5160 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      5161 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      5162 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      5163 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      5164 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      5165 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       5166 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       5167 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       5168 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       5169 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       5170 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       5171 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       5172 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       5173 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       5174 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                            m = 0                                                                     5175 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      5176 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      5177 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      5178 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      5179 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      5180 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      5181 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      5182 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      5183 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       5184 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       5185 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       5186 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       5187 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       5188 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       5189 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       5190 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       5191 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      5192 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      5193 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      5194 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     (+)-pin                                      5195 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      5196 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   (+)-pin                                      5197 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      5198 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      5199 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      5200 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      5201 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       5202 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       5203 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       5204 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 CN                                                                     OH, OH                                       5205 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       5206 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 COOH                                                                   OH, OH                                       5207 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       5208 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       5209 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       5210 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       ______________________________________                                    

                  TABLE 45                                                         ______________________________________                                          ##STR140##                                                                    Ex    X            R.sup.13   Y.sup.1 Y.sup.2                                                                        Phys. Data                               ______________________________________                                         m = 1                                                                          5215  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 (+)-pin                                          5216  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 OH, OH                                           5217  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 (+)-pin                                          5218  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 OH, OH                                           5219  OMe          PhCH.sub.2 (+)-pin                                          5220  OMe          PhCH.sub.2 OH, OH                                           5221  NH(CNH)H     PhCH.sub.2 (+)-pin                                          5222  NH(CNH)H     PhCH.sub.2 OH, OH                                           5223  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5224  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5225  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5226  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5227  OMe          PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5228  OMe          PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5229  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5230  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5231  CH.sub.2 NH.sub.2                                                                           Ph         (+)-pin                                          5232  CH.sub.2 NH.sub.2                                                                           Ph         OH, OH                                           5233  NH(CNH)NH.sub.2                                                                             Ph         (+)-pin                                          5234  NH(CNH)NH.sub.2                                                                             Ph         OH, OH                                           5235  OMe          Ph         (+)-pin                                          5236  OMe          Ph         OH, OH                                           5237  NH(CNH)H     Ph         (+)-pin                                          5238  NH(CNH)H     Ph         OH, OH                                                 m = 0                                                                    5239  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 (+)-pin                                          5240  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 OH, OH                                           5241  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 (+)-pin                                          5242  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 OH, OH                                           5243  OMe          PhCH.sub.2 (+)-pin                                          5244  OMe          PhCH.sub.2 OH, OH                                           5245  NH(CNH)H     PhCH.sub.2 (+)-pin                                          5246  NH(CNH)H     PhCH.sub.2 OH, OH                                           5247  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5248  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5249  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5250  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5251  OMe          PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5252  OMe          PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5253  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5254  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5255  CH.sub.2 NH.sub.2                                                                           Ph         (+)-pin                                          5256  CH.sub.2 NH.sub.2                                                                           Ph         OH, OH                                           5257  NH(CNH)NH.sub.2                                                                             Ph         (+)-pin                                          5258  NH(CNH)NH.sub.2                                                                             Ph         OH, OH                                           5259  OMe          Ph         (+)-pin                                          5260  OMe          Ph         OH, OH                                           5261  NH(CNH)H     Ph         (+)-pin                                          5262  NH(CNH)H     Ph         OH, OH                                           ______________________________________                                    

                  TABLE 46                                                         ______________________________________                                          ##STR141##                                                                    Ex    X            R.sup.13   Y.sup.1 Y.sup.2                                                                        Phys. Data                               ______________________________________                                         m = 1                                                                          5267  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 (+)-pin                                          5268  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 OH, OH                                           5269  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 (+)-pin                                          5270  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 OH, OH                                           5271  OMe          PhCH.sub.2 (+)-pin                                          5272  OMe          PhCH.sub.2 OH, OH                                           5273  NH(CNH)H     PhCH.sub.2 (+)-pin                                          5274  NH(CNH)H     PhCH.sub.2 OH, OH                                           5275  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5276  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5277  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5278  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5279  OMe          PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5280  OMe          PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5281  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5282  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5283  CH.sub.2 NH.sub.2                                                                           Ph         (+)-pin                                          5284  CH.sub.2 NH.sub.2                                                                           Ph         OH, OH                                           5285  NH(CNH)NH.sub.2                                                                             Ph         (+)-pin                                          5286  NH(CNH)NH.sub.2                                                                             Ph         OH, OH                                           5287  OMe          Ph         (+)-pin                                          5288  OMe          Ph         OH, OH                                           5289  NH(CNH)H     Ph         (+)-pin                                          5290  NH(CNH)H     Ph         OH, OH                                                 m = 0                                                                    5291  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 (+)-pin                                          5292  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 OH, OH                                           5293  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 (+)-pin                                          5294  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 OH, OH                                           5295  OMe          PhCH.sub.2 (+)-pin                                          5296  OMe          PhCH.sub.2 OH, OH                                           5297  NH(CNH)H     PhCH.sub.2 (+)-pin                                          5298  NH(CNH)H     PhCH.sub.2 OH, OH                                           5299  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5300  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5301  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5302  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5303  OMe          PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5304  OMe          PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5305  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5306  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5307  CH.sub.2 NH.sub.2                                                                           Ph         (+)-pin                                          5308  CH.sub.2 NH.sub.2                                                                           Ph         OH, OH                                           5309  NH(CNH)NH.sub.2                                                                             Ph         (+)-pin                                          5310  NH(CNH)NH.sub.2                                                                             Ph         OH, OH                                           5311  OMe          Ph         (+)-pin                                          5312  OMe          Ph         OH, OH                                           5313  NH(CNH)H     Ph         (+)-pin                                          5314  NH(CNH)H     Ph         OH, OH                                           ______________________________________                                    

                  TABLE 47                                                         ______________________________________                                          ##STR142##                                                                    Ex    X            R.sup.13   Y.sup.1 Y.sup.2                                                                        Phys. Data                               ______________________________________                                         m = 1                                                                          5319  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 (+)-pin                                          5320  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 OH, OH                                           5321  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 (+)-pin                                          5322  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 OH, OH                                           5323  OMe          PhCH.sub.2 (+)-pin                                          5324  OMe          PhCH.sub.2 OH, OH                                           5325  NH(CNH)H     PhCH.sub.2 (+)-pin                                          5326  NH(CNH)H     PhCH.sub.2 OH, OH                                           5327  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5328  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5329  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5330  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5331  OMe          PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5332  OMe          PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5333  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5334  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5335  CH.sub.2 NH.sub.2                                                                           Ph         (+)-pin                                          5336  CH.sub.2 NH.sub.2                                                                           Ph         OH, OH                                           5337  NH(CNH)NH.sub.2                                                                             Ph         (+)-pin                                          5338  NH(CNH)NH.sub.2                                                                             Ph         OH, OH                                           5339  OMe          Ph         (+)-pin                                          5340  OMe          Ph         OH, OH                                           5341  NH(CNH)H     Ph         (+)-pin                                          5342  NH(CNH)H     Ph         OH, OH                                                 m = 0                                                                    5343  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 (+)-pin                                          5344  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 OH, OH                                           5345  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 (+)-pin                                          5346  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 OH, OH                                           5347  OMe          PhCH.sub.2 (+)-pin                                          5348  OMe          PhCH.sub.2 OH, OH                                           5349  NH(CNH)H     PhCH.sub.2 (+)-pin                                          5350  NH(CNH)H     PhCH.sub.2 OH, OH                                           5351  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5352  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5353  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5354  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5355  OMe          PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5356  OMe          PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5357  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                          5358  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       OH, OH                                           5359  CH.sub.2 NH.sub.2                                                                           Ph         (+)-pin                                          5360  CH.sub.2 NH.sub.2                                                                           Ph         OH, OH                                           5361  NH(CNH)NH.sub.2                                                                             Ph         (+)-pin                                          5362  NH(CNH)NH.sub.2                                                                             Ph         OH, OH                                           5363  OMe          Ph         (+)-pin                                          5364  OMe          Ph         OH, OH                                           5365  NH(CNH)H     Ph         (+)-pin                                          5366  NH(CNH)H     Ph         OH, OH                                           ______________________________________                                    

                                      TABLE 48                                     __________________________________________________________________________      ##STR143##                                                                                                         Phys.                                     Ex X       R.sup.13                                                                           R.sup.14                                                                             R.sup.15   Y.sup.1 Y.sup.2                                                                     Data                                      __________________________________________________________________________     5371                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     H          (+)-pin                                        5372                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     methyl     (+)-pin                                        5373                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 CN                                                                               (+)-pin                                        5374                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 COOH                                                                             (+)-pin                                        5375                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 NC                                                                               (+)-pin                                        5376                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 NO.sub.2                                                                         (+)-pin                                        5377                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     (CH.sub.2).sub.2 OH                                                                       (+)-pin                                        5378                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 SOCH.sub.3                                                                       (+)-pin                                        5379                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     H          OH, OH                                         5380                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     methyl     OH, OH                                         5381                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 CN                                                                               OH, OH                                         5382                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 COOH                                                                             OH, OH                                         5383                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 NC                                                                               OH, OH                                         5384                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 NO.sub.2                                                                         OH, OH                                         5385                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     (CH.sub.2).sub.2 OH                                                                       OH, OH                                         5386                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 SOCH.sub.3                                                                       OH, OH                                         5387                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     H          (+)-pin                                        5388                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     methyl     (+)-pin                                        5389                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 CN                                                                               (+)-pin                                        5390                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 COOH                                                                             (+)-pin                                        5391                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 NC                                                                               (+)-pin                                        5392                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 NO.sub.2                                                                         (+)-pin                                        5393                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     (CH.sub.2).sub.2 OH                                                                       (+)-pin                                        5394                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 SOCH.sub.3                                                                       (+)-pin                                        5395                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     H          OH, OH                                         5396                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     methyl     OH, OH                                         5397                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 CN                                                                               OH, OH                                         5398                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 COOH                                                                             OH, OH                                         5399                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 NC                                                                               OH, OH                                         5400                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 NO.sub.2                                                                         OH, OH                                         5401                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     (CH.sub.2).sub.2 OH                                                                       OH, OH                                         5402                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 SOCH.sub.3                                                                       OH, OH                                         5403                                                                              m = 0                                                                       5404                                                                              NH(CNH)NH.sub.2                                                                        H   H     3-(t-butyl-O.sub.2 CNH)-Ph                                                                (+)-pin                                                                             BS                                        5405                                                                              NH(CNH)NH.sub.2                                                                        H   H     3-(t-butyl-O.sub.2 CNH)-Ph                                                                OH, OH                                         5406                                                                              NH(CNH)NH.sub.2                                                                        H   H     3-(NH.sub.2)-Ph                                                                           (+)-pin                                        5407                                                                              NH(CNH)NH.sub.2                                                                        H   H     3-(NH.sub.2)-Ph                                                                           OH, OH                                         5408                                                                              NH(CNH)NH.sub.2                                                                        H   H     3-(CH.sub.3 SO.sub.2 NH)-Ph                                                               (+)-pin                                        5409                                                                              NH(CNH)NH.sub.2                                                                        H   H     3-(CH.sub.3 SO.sub.2 NH)-Ph                                                               OH, OH                                         5410                                                                              NH(CNH)NH.sub.2                                                                        H   methyl                                                                               Ph         (+)-pin                                        5411                                                                              NH(CNH)NH.sub.2                                                                        H   methyl                                                                               Ph         OH, OH                                         5412                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.2 CN                                                                          Ph         (+)-pin                                        5413                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.2 CN                                                                          Ph         OH, OH                                         5414                                                                              NH(CNH)NH.sub.2                                                                        H   methyl                                                                               3-(CH.sub.3 SO.sub.2 NH)-Ph                                                               (+)-pin                                        5415                                                                              NH(CNH)NH.sub.2                                                                        H   methyl                                                                               3-(CH.sub.3 SO.sub.2 NH)-Ph                                                               OH, OH                                         5416                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.3                                                                             2-(CH.sub.3 SO.sub.2 NH)-Ph                                                               (+)-pin                                        5417                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.3                                                                             2-(CH.sub.3 SO.sub.2 NH)-Ph                                                               OH, OH                                         5418                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.2 CN                                                                          3-(CH.sub.3 SO.sub.2 NH)-Ph                                                               (+)-pin                                        5419                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.2 CN                                                                          3-(CH.sub.3 SO.sub.2 NH)-Ph                                                               OH, OH                                         5420                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.2 CN                                                                          2-(CH.sub.3 SO.sub.2 NH)-Ph                                                               (+)-pin                                        5421                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.2 CN                                                                          2-(CH.sub.3 SO.sub.2 NH)-Ph                                                               OH, OH                                         5422                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.2 COOH                                                                        3-(CH.sub.3 SO.sub.2 NH)-Ph                                                               (+)-pin                                        5423                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.2 COOH                                                                        3-(CH.sub.3 SO.sub.2 NH)-Ph                                                               OH, OH                                         5424                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.2 COOH                                                                        2-(CH.sub.3 SO.sub.2 NH)-Ph                                                               (+)-pin                                        5425                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.2 COOH                                                                        2-(CH.sub.3 SO.sub.2 NH)-Ph                                                               OH, OH                                         5426                                                                              NH(CNH)NH.sub.2                                                                        H   H     3-(t-butylOCONH)-Ph                                                                       (+)-pin                                                                             BP                                        __________________________________________________________________________      BP. MS (M+H)+: Calc 610, Found 610.                                            BS. MS (M+H)+: Calc 610, Found 610.                                      

                  TABLE 49                                                         ______________________________________                                          ##STR144##                                                                                                             Phys.                                 Ex   X           R.sup.13                                                                               R.sup.14 Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         m = 1                                                                          5431 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      5432 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      5433 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      5434 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      5435 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      5436 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      5437 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      5438 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      5439 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       5440 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       5441 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       5442 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       5443 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       5444 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       5445 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       5446 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       5447 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      5448 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      5449 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      5450 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      5451 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      5452 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      5453 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      5454 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      5455 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       5456 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       5457 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       5458 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       5459 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       5460 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       5461 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       5462 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                            m = 0                                                                     5463 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        (+)-pin                                      5464 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   (+)-pin                                      5465 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      5466 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      5465 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      5466 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      5467 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      5468 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      5469 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             H        OH, OH                                       5470 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             methyl   OH, OH                                       5471 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       5472 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       5473 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       5474 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       5475 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       5476 CH.sub.2 NH.sub.2                                                                          PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       5477 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        (+)-pin                                      5478 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   (+)-pin                                      5479 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             (+)-pin                                      5480 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           (+)-pin                                      5481 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             (+)-pin                                      5482 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       (+)-pin                                      5483 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     (+)-pin                                      5484 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     (+)-pin                                      5485 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             H        OH, OH                                       5486 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             methyl   OH, OH                                       5487 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 CN                                                                             OH, OH                                       5488 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 COOH                                                                           OH, OH                                       5489 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NC                                                                             OH, OH                                       5490 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 NO.sub.2                                                                       OH, OH                                       5491 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             (CH.sub.2).sub.2 OH                                                                     OH, OH                                       5492 NH(CNH)NH.sub.2                                                                            PhCH.sub.2                                                                             CH.sub.2 SOCH.sub.3                                                                     OH, OH                                       ______________________________________                                    

                                      TABLE 50                                     __________________________________________________________________________      ##STR145##                                                                                                         Phys.                                     Ex X       R.sup.13                                                                           R.sup.14                                                                             R.sup.15   Y.sup.1 Y.sup.2                                                                     Data                                      __________________________________________________________________________     5497                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     H          (+)-pin                                        5498                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     methyl     (+)-pin                                        5499                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 CN                                                                               (+)-pin                                        5500                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 COOH                                                                             (+)-pin                                        5501                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 NC                                                                               (+)-pin                                        5502                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 NO.sub.2                                                                         (+)-pin                                        5503                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     (CH.sub.2).sub.2 OH                                                                       (+)-pin                                        5504                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 SOCH.sub.3                                                                       (+)-pin                                        5505                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     H          OH, OH                                         5506                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     methyl     OH, OH                                         5507                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 CN                                                                               OH, OH                                         5508                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 COOH                                                                             OH, OH                                         5509                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 NC                                                                               OH, OH                                         5510                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 NO.sub.2                                                                         OH, OH                                         5511                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     (CH.sub.2).sub.2 OH                                                                       OH, OH                                         5512                                                                              CH.sub.2 NH.sub.2                                                                      PhCH.sub.2                                                                         H     CH.sub.2 SOCH.sub.3                                                                       OH, OH                                         5513                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     H          (+)-pin                                        5514                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     methyl     (+)-pin                                        5515                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 CN                                                                               (+)-pin                                        5516                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 COOH                                                                             (+)-pin                                        5517                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 NC                                                                               (+)-pin                                        5518                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 NO.sub.2                                                                         (+)-pin                                        5519                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     (CH.sub.2).sub.2 OH                                                                       (+)-pin                                        5520                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 SOCH.sub.3                                                                       (+)-pin                                        5521                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     H          OH, OH                                         5522                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     methyl     OH, OH                                         5523                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 CN                                                                               OH, OH                                         5524                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 COOH                                                                             OH, OH                                         5525                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 NC                                                                               OH, OH                                         5526                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 NO.sub.2                                                                         OH, OH                                         5527                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     (CH.sub.2).sub.2 OH                                                                       OH, OH                                         5528                                                                              NH(CNH)NH.sub.2                                                                        PhCH.sub.2                                                                         H     CH.sub.2 SOCH.sub.3                                                                       OH, OH                                            m = 0                                                                       5529                                                                              NH(CNH)NH.sub.2                                                                        H   H     3-(t-butyl-O.sub.2 CNH)-Ph                                                                (+)-pin                                                                             BT                                        5530                                                                              NH(CNH)NH.sub.2                                                                        H   H     3-(t-butyl-O.sub.2 CNH)-Ph                                                                OH, OH                                         5531                                                                              NH(CNH)NH.sub.2                                                                        H   H     3-(NH.sub.2)-Ph                                                                           (+)-pin                                        5532                                                                              NH(CNH)NH.sub.2                                                                        H   H     3-(NH.sub.2)-Ph                                                                           OH, OH                                         5533                                                                              NH(CNH)NH.sub.2                                                                        H   H     3-(CH.sub.3 SO.sub.2 NH)-Ph                                                               (+)-pin                                        5534                                                                              NH(CNH)NH.sub.2                                                                        H   H     3-(CH.sub.3 SO.sub.2 NH)-Ph                                                               OH, OH                                         5535                                                                              NH(CNH)NH.sub.2                                                                        H   H     Ph         (+)-pin                                                                             BU                                        5536                                                                              NH(CNH)NH.sub.2                                                                        H   H     Ph         OH, OH                                                                              BV                                        5537                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.3                                                                             Ph         (+)-pin                                        5538                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.3                                                                             Ph         OH, OH                                         5539                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.2 CN                                                                          Ph         (+)-pin                                        5540                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.2 CN                                                                          Ph         OH, OH                                         5541                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.2 COOH                                                                        Ph         (+)-pin                                        5542                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.2 COOH                                                                        Ph         OH, OH                                         5543                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.2 SO.sub.2 NH.sub.2                                                           Ph         (+)-pin                                        5544                                                                              NH(CNH)NH.sub.2                                                                        H   CH.sub.2 SO.sub.2 NH.sub.2                                                           Ph         OH, OH                                         5545                                                                              NH(CNH)NH                                                                              H   CH.sub.2 CN                                                                          3-(CH.sub.3 SO.sub.2 NH)-Ph                                                               (+)-pin                                        5546                                                                              NH(CNH)NH                                                                              H   CH.sub.2 CN                                                                          3-(CH.sub.3 SO.sub.2 NH)-Ph                                                               OH, OH                                         5547                                                                              NH(CNH)NH                                                                              H   CH.sub.2 COOH                                                                        3-(CH.sub.3 SO.sub.2 NH)-Ph                                                               (+)-pin                                        5548                                                                              NH(CNH)NH                                                                              H   CH.sub.2 COOH                                                                        3-(CH.sub.3 SO.sub.2 NH)-Ph                                                               OH, OH                                         5549                                                                              NH(CNH)NH                                                                              H   CH.sub.2 COOH                                                                        2-(CH.sub.3 SO.sub.2 NH)-Ph                                                               (+)-pin                                        5550                                                                              NH(CNH)NH                                                                              H   CH.sub.2 COOH                                                                        2-(CH.sub.3 SO.sub.2 NH)-Ph                                                               OH, OH                                         5551                                                                              NH(CNH)NH.sub.2                                                                        H   H     3-(t-butylOCONH)-Ph                                                                       (+)-pin                                                                             BO                                        5552                                                                              NH(CNH)NH.sub.2                                                                        H   H     Ph         (+)-pin                                                                             BQ                                        5553                                                                              NH(CNH)NH.sub.2                                                                        H   H     Ph         OH   BR                                        __________________________________________________________________________      BO. MS (M+H).sup.+ : Calc. 594, Found 594.                                     BQ. MS (M+H).sup.+ : Calc. 479, Found 479.                                     BS. MS (M+H).sup.+ : Calc. 345, Found 345.                                     BT. MS (M+H).sup.+ : Calc. 594, Found 594.                                     BU. MS (M+H).sup.+ : Calc. 479, Found 479.                                     BV. MS (M+H).sup.+ : Calc. 345, Found 345.                               

                                      TABLE 51                                     __________________________________________________________________________      ##STR146##                                                                                                      Phys.                                        Ex  X        R.sup.13                                                                            R.sup.14                                                                           R.sup.15                                                                              Y.sup.1 Y.sup.2                                                                     Data                                         __________________________________________________________________________     m = 1                                                                          5558                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   H      (+)-pin                                           5559                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   methyl (+)-pin                                           5560                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 CN                                                                           (+)-pin                                           5561                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 COOH                                                                         (+)-pin                                           5562                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 NC                                                                           (+)-pin                                           5563                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 NO.sub.2                                                                     (+)-pin                                           5564                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   (CH.sub.2).sub.2 OH                                                                   (+)-pin                                           5565                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                           5566                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   H      OH, OH                                            5567                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   methyl OH, OH                                            5568                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 CN                                                                           OH, OH                                            5569                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 COOH                                                                         OH, OH                                            5570                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 NC                                                                           OH, OH                                            5571                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 NO.sub.2                                                                     OH, OH                                            5572                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   (CH.sub.2).sub.2 OH                                                                   OH, OH                                            5573                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 SOCH.sub.3                                                                   OH, OH                                            5574                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   H      (+)-pin                                           5575                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   methyl (+)-pin                                           5576                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 CN                                                                           (+)-pin                                           5577                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 COOH                                                                         (+)-pin                                           5578                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 NC                                                                           (+)-pin                                           5579                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 NO.sub.2                                                                     (+)-pin                                           5580                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   (CH.sub.2).sub.2 OH                                                                   (+)-pin                                           5581                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                           5582                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   H      OH, OH                                            5583                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   methyl OH, OH                                            5584                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 CN                                                                           OH, OH                                            5585                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 COOH                                                                         OH, OH                                            5586                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 NC                                                                           OH, OH                                            5587                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 NO.sub.2                                                                     OH, OH                                            5588                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   (CH.sub.2).sub.2 OH                                                                   OH, OH                                            5589                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 SOCH.sub.3                                                                   OH, OH                                            m = 0                                                                          5590                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   H      (+)-pin                                           5591                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   methyl (+)-pin                                           5592                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 CN                                                                           (+)-pin                                           5593                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 COOH                                                                         (+)-pin                                           5594                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 NC                                                                           (+)-pin                                           5595                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 NO.sub.2                                                                     (+)-pin                                           5596                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   (CH.sub.2).sub.2 OH                                                                   (+)-pin                                           5597                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                           5598                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   H      OH, OH                                            5599                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   methyl OH, OH                                            5600                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 CN                                                                           OH, OH                                            5601                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 COOH                                                                         OH, OH                                            5602                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 NC                                                                           OH, OH                                            5603                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 NO.sub.2                                                                     OH, OH                                            5604                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   (CH.sub.2).sub.2 OH                                                                   OH, OH                                            5605                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H   CH.sub.2 SOCH.sub.3                                                                   OH, OH                                            5606                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   H      (+)-pin                                           5607                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   methyl (+)-pin                                           5608                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 CN                                                                           (+)-pin                                           5609                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 COOH                                                                         (+)-pin                                           5610                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 NC                                                                           (+)-pin                                           5611                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 NO.sub.2                                                                     (+)-pin                                           5612                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   (CH.sub.2).sub.2 OH                                                                   (+)-pin                                           5613                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                           5614                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   H      OH, OH                                            5615                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   methyl OH, OH                                            5616                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 CN                                                                           OH, OH                                            5617                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 COOH                                                                         OH, OH                                            5618                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 NC                                                                           OH, OH                                            5619                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 NO.sub.2                                                                     OH, OH                                            5620                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   (CH.sub.2).sub.2 OH                                                                   OH, OH                                            5621                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H   CH.sub.2 SOCH.sub.3                                                                   OH, OH                                            __________________________________________________________________________

                                      TABLE 52                                     __________________________________________________________________________      ##STR147##                                                                    Ex X        R.sup.13                                                                              R.sup.14                                                                               Y.sup.1 Y.sup.2                                                                     Phys. Data                                     __________________________________________________________________________     m = 1                                                                          5626                                                                              CH.sub.2 NH.sub.2                                                                       H      H       (+)-pin                                             5627                                                                              CH.sub.2 NH.sub.2                                                                       H      methyl  (+)-pin                                             5628                                                                              CH.sub.2 NH.sub.2                                                                       H      H       OH, OH                                              5629                                                                              CH.sub.2 NH.sub.2                                                                       H      methyl  OH, OH                                              5630                                                                              CH.sub.2 NH.sub.2                                                                       H      CH.sub.2 CN                                                                            (+)-pin                                             5631                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                             5632                                                                              CH.sub.2 NH.sub.2                                                                       H      CH.sub.2 CN                                                                            OH, OH                                              5633                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2 ).sub.2 COOH                                                                 OH, OH                                              5634                                                                              CH.sub.2 NH.sub.2                                                                       H      CH.sub.2 COOMe                                                                         (+)-pin                                             5635                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2)COOH                                                                         (+)-pin                                             5636                                                                              CH.sub.2 NH.sub.2                                                                       H      CH.sub.2 COOMe                                                                         OH, OH                                              5637                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2)COOH                                                                         OH, OH                                              5638                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2).sub.2 CN.sub.4 H                                                            (+)-pin                                             5639                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2)CN.sub.4 H                                                                   (+)-pin                                             5640                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2).sub.2 CN.sub.4 H                                                            OH, OH                                              5641                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2)CN.sub.4 H                                                                   OH, OH                                              5642                                                                              NH(CNH)NH.sub.2                                                                         H      H       (+)-pin                                             5643                                                                              NH(CNH)NH.sub.2                                                                         H      methyl  (+)-pin                                             5644                                                                              NH(CNH)NH.sub.2                                                                         H      H       OH, OH                                              5645                                                                              NH(CNH)NH.sub.2                                                                         H      methyl  OH, OH                                              5646                                                                              NH(CNH)NH.sub.2                                                                         H      CH.sub.2 CN                                                                            (+)-pin                                             5647                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                             5648                                                                              NH(CNH)NH.sub.2                                                                         H      CH.sub.2 CN                                                                            OH, OH                                              5649                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2 ).sub.2 COOH                                                                 OH, OH                                              5650                                                                              NH(CNH)NH.sub.2                                                                         H      CH.sub.2 COOMe                                                                         (+)-pin                                             5651                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2)COOH                                                                         (+)-pin                                             5652                                                                              NH(CNH)NH.sub.2                                                                         H      CH.sub.2 COOMe                                                                         OH, OH                                              5653                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2)COOH                                                                         OH, OH                                              5654                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2).sub.2 CN.sub.4 H                                                            (+)-pin                                             5655                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2)CN.sub.4 H                                                                   (+)-pin                                             5656                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2).sub.2 CN.sub.4 H                                                            OH, OH                                              5657                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2)CN.sub.4 H                                                                   OH, OH                                              5658                                                                              OMe      H      H       (+)-pin                                             5659                                                                              OMe      H      H       OH, OH                                              5660                                                                              NH(CNH)H H      H       (+)-pin                                             5661                                                                              NH(CNH)H H      H       OH, OH                                              5662                                                                              CH.sub.2 NH.sub.2                                                                       CH.sub.2 CN                                                                           H       (+)-pin                                             5663                                                                              CH.sub.2 NH.sub.2                                                                       CH.sub.2 CN                                                                           H       OH, OH                                              5664                                                                              NH(CNH)NH.sub.2                                                                         (CH.sub.2).sub.2 COOH                                                                 H       (+)-pin                                             5665                                                                              NH(CNH)NH.sub.2                                                                         (CH.sub.2).sub.2 COOH                                                                 H       OH, OH                                              5666                                                                              OMe      CH.sub.2 COOMe                                                                        H       (+)-pin                                             5667                                                                              OMe      CH.sub.2 COOMe                                                                        H       OH, OH                                              5668                                                                              NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H                                                           H       OH, OH                                              5669                                                                              NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H                                                           H       (+)-pin                                             m = 1                                                                          5670                                                                              CH.sub.2 NH.sub.2                                                                       H      H       (+)-pin                                             5671                                                                              CH.sub.2 NH.sub.2                                                                       H      methyl  (+)-pin                                             5672                                                                              CH.sub.2 NH.sub.2                                                                       H      H       OH, OH                                              5673                                                                              CH.sub.2 NH.sub.2                                                                       H      methyl  OH, OH                                              5674                                                                              CH.sub.2 NH.sub.2                                                                       H      CH.sub.2 CN                                                                            (+)-pin                                             5675                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                             5676                                                                              CH.sub.2 NH.sub.2                                                                       H      CH.sub.2 CN                                                                            OH, OH                                              5677                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2 ).sub.2 COOH                                                                 OH, OH                                              5678                                                                              CH.sub.2 NH.sub.2                                                                       H      CH.sub.2 COOMe                                                                         (+)-pin                                             5679                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2)COOH                                                                         (+)-pin                                             5680                                                                              CH.sub.2 NH.sub.2                                                                       H      CH.sub.2 COOMe                                                                         OH, OH                                              5681                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2)COOH                                                                         OH, OH                                              5682                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2).sub.2 CN.sub.4 H                                                            (+)-pin                                             5683                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2)CN.sub.4 H                                                                   (+)-pin                                             5684                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2).sub.2 CN.sub.4 H                                                            OH, OH                                              5685                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2)CN.sub.4 H                                                                   OH, OH                                              5686                                                                              NH(CNH)NH.sub.2                                                                         H      H       (+)-pin                                             5687                                                                              NH(CNH)NH.sub.2                                                                         H      methyl  (+)-pin                                             5688                                                                              NH(CNH)NH.sub.2                                                                         H      H       OH, OH                                              5689                                                                              NH(CNH)NH.sub.2                                                                         H      methyl  OH, OH                                              5690                                                                              NH(CNH)NH.sub.2                                                                         H      CH.sub.2 CN                                                                            (+)-pin                                             5691                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                             5692                                                                              NH(CNH)NH.sub.2                                                                         H      CH.sub.2 CN                                                                            OH, OH                                              5693                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2 ).sub.2 COOH                                                                 OH, OH                                              5694                                                                              NH(CNH)NH.sub.2                                                                         H      CH.sub.2 COOMe                                                                         (+)-pin                                             5695                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2)COOH                                                                         (+)-pin                                             5696                                                                              NH(CNH)NH.sub.2                                                                         H      CH.sub.2 COOMe                                                                         OH, OH                                              5697                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2)COOH                                                                         OH, OH                                              5698                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2).sub.2 CN.sub.4 H                                                            (+)-pin                                             5699                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2)CN.sub.4 H                                                                   (+)-pin                                             5700                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2).sub.2 CN.sub.4 H                                                            OH, OH                                              5701                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2)CN.sub.4 H                                                                   OH, OH                                              5702                                                                              OMe      H      H       (+)-pin                                             5703                                                                              OMe      H      H       OH, OH                                              5704                                                                              NH(CNH)H H      H       (+)-pin                                             5705                                                                              NH(CNH)H H      H       OH, OH                                              5706                                                                              CH.sub.2 NH.sub.2                                                                       CH.sub.2 CN                                                                           H       (+)-pin                                             5707                                                                              CH.sub.2 NH.sub.2                                                                       CH.sub.2 CN                                                                           H       OH, OH                                              5708                                                                              NH(CNH)NH.sub.2                                                                         (CH.sub.2).sub.2 COOH                                                                 H       (+)-pin                                             5709                                                                              NH(CNH)NH.sub.2                                                                         (CH.sub.2).sub.2 COOH                                                                 H       OH, OH                                              5710                                                                              OMe      CH.sub.2 COOMe                                                                        H       (+)-pin                                             5711                                                                              OMe      CH.sub.2 COOMe                                                                        H       OH, OH                                              5712                                                                              NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H                                                           H       OH, OH                                              5713                                                                              NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H                                                           H       (+)-pin                                             m = 0                                                                          5714                                                                              CH.sub.2 NH.sub.2                                                                       H      H       (+)-pin                                             5715                                                                              CH.sub.2 NH.sub.2                                                                       H      methyl  (+)-pin                                             5716                                                                              CH.sub.2 NH.sub.2                                                                       H      H       OH, OH                                              5717                                                                              CH.sub.2 NH.sub.2                                                                       H      methyl  OH, OH                                              5718                                                                              CH.sub.2 NH.sub.2                                                                       H      CH.sub.2 CN                                                                            (+)-pin                                             5719                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                             5720                                                                              CH.sub.2 NH.sub.2                                                                       H      CH.sub.2 CN                                                                            OH, OH                                              5721                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2 ).sub.2 COOH                                                                 OH, OH                                              5722                                                                              CH.sub.2 NH.sub.2                                                                       H      CH.sub.2 COOMe                                                                         (+)-pin                                             5723                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2)COOH                                                                         (+)-pin                                             5724                                                                              CH.sub.2 NH.sub.2                                                                       H      CH.sub.2 COOMe                                                                         OH, OH                                              5725                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2)COOH                                                                         OH, OH                                              5726                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2).sub.2 CN.sub.4 H                                                            (+)-pin                                             5727                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2)CN.sub.4 H                                                                   (+)-pin                                             5728                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2).sub.2 CN.sub.4 H                                                            OH, OH                                              5729                                                                              CH.sub.2 NH.sub.2                                                                       H      (CH.sub.2)CN.sub.4 H                                                                   OH, OH                                              5730                                                                              NH(CNH)NH.sub.2                                                                         H      H       (+)-pin                                             5731                                                                              NH(CNH)NH.sub.2                                                                         H      methyl  (+)-pin                                             5732                                                                              NH(CNH)NH.sub.2                                                                         H      H       OH, OH                                              5733                                                                              NH(CNH)NH.sub.2                                                                         H      methyl  OH, OH                                              5734                                                                              NH(CNH)NH.sub.2                                                                         H      CH.sub.2 CN                                                                            (+)-pin                                             5735                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                             5736                                                                              NH(CNH)NH.sub.2                                                                         H      CH.sub.2 CN                                                                            OH, OH                                              5737                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2 ).sub.2 COOH                                                                 OH, OH                                              5738                                                                              NH(CNH)NH.sub.2                                                                         H      CH.sub.2 COOMe                                                                         (+)-pin                                             5739                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2)COOH                                                                         (+)-pin                                             5740                                                                              NH(CNH)NH.sub.2                                                                         H      CH.sub.2 COOMe                                                                         OH, OH                                              5741                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2)COOH                                                                         OH, OH                                              5742                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2).sub.2 CN.sub.4 H                                                            (+)-pin                                             5743                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2)CN.sub.4 H                                                                   (+)-pin                                             5744                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2).sub.2 CN.sub.4 H                                                            OH, OH                                              5745                                                                              NH(CNH)NH.sub.2                                                                         H      (CH.sub.2)CN.sub.4 H                                                                   OH, OH                                              5746                                                                              OMe      H      H       (+)-pin                                             5747                                                                              OMe      H      H       OH, OH                                              5748                                                                              NH(CNH)H H      H       (+)-pin                                             5749                                                                              NH(CNH)H H      H       OH, OH                                              5750                                                                              CH.sub.2 NH.sub.2                                                                       CH.sub.2 CN                                                                           H       (+)-pin                                             5751                                                                              CH.sub.2 NH.sub.2                                                                       CH.sub.2 CN                                                                           H       OH, OH                                              5752                                                                              NH(CNH)NH.sub.2                                                                         (CH.sub.2).sub.2 COOH                                                                 H       (+)-pin                                             5753                                                                              NH(CNH)NH.sub.2                                                                         (CH.sub.2).sub.2 COOH                                                                 H       OH, OH                                              5754                                                                              OMe      CH.sub.2 COOMe                                                                        H       (+)-pin                                             5755                                                                              OMe      CH.sub.2 COOMe                                                                        H       OH, OH                                              5756                                                                              NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H                                                           H       OH, OH                                              5757                                                                              NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H                                                           H       (+)-pin                                             __________________________________________________________________________

                  TABLE 53                                                         ______________________________________                                          ##STR148##                                                                    Ex   X           R.sup.13  R.sup.14                                                                            Y.sup.1 Y.sup.2                                                                       Phys. Data                              ______________________________________                                         5762 CH.sub.2 NH.sub.2                                                                          H         H    (+)-pin                                        5763 CH.sub.2 NH.sub.2                                                                          H         H    OH, OH                                         5764 NH(CNH)NH.sub.2                                                                            H         H    (+)-pin                                        5765 NH(CNH)NH.sub.2                                                                            H         H    OH, OH                                         5766 OMe         H         H    (+)-pin                                        5767 OMe         H         H    OH, OH                                         5768 NH(CNH)H    H         H    OH, OH                                         5769 NH(CNH)H    H         H    (+)-pin                                        5770 CH.sub.2 NH.sub.2                                                                          CH.sub.2 CN                                                                              H    (+)-pin                                        5771 CH.sub.2 NH.sub.2                                                                          CH.sub.2 CN                                                                              H    OH, OH                                         5772 NH(CNH)NH.sub.2                                                                            (CH.sub.2)COOH                                                                           H    (+)-pin                                        5773 NH(CNH)NH.sub.2                                                                            (CH.sub.2)COOH                                                                           H    OH, OH                                         5774 OMe         CH.sub.2 COOMe                                                                           H    (+)-pin                                        5775 OMe         CH.sub.2 COOMe                                                                           H    OH, OH                                         5776 NH(CNH)H    (CH.sub.2)CN.sub.4 H                                                                     H    OH, OH                                         5777 NH(CNH)H    (CH.sub.2)CN.sub.4 H                                                                     H    (+)-pin                                        ______________________________________                                    

                  TABLE 54                                                         ______________________________________                                          ##STR149##                                                                    Ex   X           R.sup.13  R.sup.14                                                                            Y.sup.1 Y.sup.2                                                                       Phys. Data                              ______________________________________                                         5782 CH.sub.2 NH.sub.2                                                                          H         H    (+)-pin                                        5783 CH.sub.2 NH.sub.2                                                                          H         H    OH, OH                                         5784 NH(CNH)NH.sub.2                                                                            H         H    (+)-pin                                        5785 NH(CNH)NH.sub.2                                                                            H         H    OH, OH                                         5786 OMe         H         H    (+)-pin                                        5787 OMe         H         H    OH, OH                                         5788 NH(CNH)H    H         H    OH, OH                                         5789 NH(CNH)H    H         H    (+)-pin                                        5790 CH.sub.2 NH.sub.2                                                                          CH.sub.2 CN                                                                              H    (+)-pin                                        5791 CH.sub.2 NH.sub.2                                                                          CH.sub.2 CN                                                                              H    OH, OH                                         5792 NH(CNH)NH.sub.2                                                                            (CH.sub.2)COOH                                                                           H    (+)-pin                                        5793 NH(CNH)NH.sub.2                                                                            (CH.sub.2)COOH                                                                           H    OH, OH                                         5794 OMe         CH.sub.2 COOMe                                                                           H    (+)-pin                                        5795 OMe         CH.sub.2 COOMe                                                                           H    OH, OH                                         5796 NH(CNH)H    (CH.sub.2)CN.sub.4 H                                                                     H    OH, OH                                         5797 NH(CNH)H    (CH.sub.2)CN.sub.4 H                                                                     H    (+)-pin                                        ______________________________________                                    

                  TABLE 55                                                         ______________________________________                                          ##STR150##                                                                    Ex   X           R.sup.13  R.sup.14                                                                            Y.sup.1 Y.sup.2                                                                       Phys. Data                              ______________________________________                                         5802 CH.sub.2 NH.sub.2                                                                          H         H    (+)-pin                                        5803 CH.sub.2 NH.sub.2                                                                          H         H    OH, OH                                         5804 NH(CNH)NH.sub.2                                                                            H         H    (+)-pin                                        5805 NH(CNH)NH.sub.2                                                                            H         H    OH, OH                                         5806 OMe         H         H    (+)-pin                                        5807 OMe         H         H    OH, OH                                         5808 NH(CNH)H    H         H    OH, OH                                         5809 NH(CNH)H    H         H    (+)-pin                                        5810 CH.sub.2 NH.sub.2                                                                          CH.sub.2 CN                                                                              H    (+)-pin                                        5811 CH.sub.2 NH.sub.2                                                                          CH.sub.2 CN                                                                              H    OH, OH                                         5812 NH(CNH)NH.sub.2                                                                            (CH.sub.2)COOH                                                                           H    (+)-pin                                        5813 NH(CNH)NH.sub.2                                                                            (CH.sub.2)COOH                                                                           H    OH, OH                                         5814 OMe         CH.sub.2 COOMe                                                                           H    (+)-pin                                        5815 OMe         CH.sub.2 COOMe                                                                           H    OH, OH                                         5816 NH(CNH)H    (CH.sub.2)CN.sub.4 H                                                                     H    OH, OH                                         5817 NH(CNH)H    (CH.sub.2)CN.sub.4 H                                                                     H    (+)-pin                                        ______________________________________                                    

                  TABLE 56                                                         ______________________________________                                          ##STR151##                                                                    Ex   X           R.sup.13  R.sup.14                                                                            Y.sup.1 Y.sup.2                                                                       Phys. Data                              ______________________________________                                         5822 CH.sub.2 NH.sub.2                                                                          H         H    (+)-pin                                        5823 CH.sub.2 NH.sub.2                                                                          H         H    OH, OH                                         5824 NH(CNH)NH.sub.2                                                                            H         H    (+)-pin                                        5825 NH(CNH)NH.sub.2                                                                            H         H    OH, OH                                         5826 OMe         H         H    (+)-pin                                        5827 OMe         H         H    OH, OH                                         5828 NH(CNH)H    H         H    OH, OH                                         5829 NH(CNH)H    H         H    (+)-pin                                        5830 CH.sub.2 NH.sub.2                                                                          CH.sub.2 CN                                                                              H    (+)-pin                                        5831 CH.sub.2 NH.sub.2                                                                          CH.sub.2 CN                                                                              H    OH, OH                                         5832 NH(CNH)NH.sub.2                                                                            (CH.sub.2)COOH                                                                           H    (+)-pin                                        5833 NH(CNH)NH.sub.2                                                                            (CH.sub.2)COOH                                                                           H    OH, OH                                         5834 OMe         CH.sub.2 COOMe                                                                           H    (+)-pin                                        5835 OMe         CH.sub.2 COOMe                                                                           H    OH, OH                                         5836 NH(CNH)H    (CH.sub.2)CN.sub.4 H                                                                     H    OH, OH                                         5837 NH(CNH)H    (CH.sub.2)CN.sub.4 H                                                                     H    (+)-pin                                        ______________________________________                                    

                  TABLE 57                                                         ______________________________________                                          ##STR152##                                                                    Ex   X           R.sup.13  R.sup.14                                                                            Y.sup.1 Y.sup.2                                                                       Phys. Data                              ______________________________________                                         m = 1                                                                          5842 CH.sub.2 NH.sub.2                                                                          H         H    (+)-pin                                        5843 CH.sub.2 NH.sub.2                                                                          H         H    OH, OH                                         5844 NH(CNH)NH.sub.2                                                                            H         H    (+)-pin                                        5845 NH(CNH)NH.sub.2                                                                            H         H    OH, OH                                         5846 OMe         H         H    (+)-pin                                        5847 OMe         H         H    OH, OH                                         5848 NH(CNH)H    H         H    OH, OH                                         5849 NH(CNH)H    H         H    (+)-pin                                        5850 CH.sub.2 NH.sub.2                                                                          CH.sub.2 CN                                                                              H    (+)-pin                                        5851 CH.sub.2 NH.sub.2                                                                          CH.sub.2 CN                                                                              H    OH, OH                                         5852 NH(CNH)NH.sub.2                                                                            (CH.sub.2)COOH                                                                           H    (+)-pin                                        5853 NH(CNH)NH.sub.2                                                                            (CH.sub.2)COOH                                                                           H    OH, OH                                         5854 OMe         CH.sub.2 COOMe                                                                           H    (+)-pin                                        5855 OMe         CH.sub.2 COOMe                                                                           H    OH, OH                                         5856 NH(CNH)H    (CH.sub.2)CN.sub.4 H                                                                     H    OH, OH                                         5857 NH(CNH)H    (CH.sub.2)CN.sub.4 H                                                                     H    (+)-pin                                        m = 0                                                                          5858 CH.sub.2 NH.sub.2                                                                          H         H    (+)-pin                                        5859 CH.sub.2 NH.sub.2                                                                          H         H    OH, OH                                         5860 NH(CNH)NH.sub.2                                                                            H         H    (+)-pin                                        5861 NH(CNH)NH.sub.2                                                                            H         H    OH, OH                                         5862 OMe         H         H    (+)-pin                                        5863 OMe         H         H    OH, OH                                         5864 NH(CNH)H    H         H    OH, OH                                         5865 NH(CNH)H    H         H    (+)-pin                                        5866 CH.sub.2 NH.sub.2                                                                          CH.sub.2 CN                                                                              H    (+)-pin                                        5867 CH.sub.2 NH.sub.2                                                                          CH.sub.2 CN                                                                              H    OH, OH                                         5868 NH(CNH)NH.sub.2                                                                            (CH.sub.2)COOH                                                                           H    (+)-pin                                        5869 NH(CNH)NH.sub.2                                                                            (CH.sub.2)COOH                                                                           H    OH, OH                                         5870 OMe         CH.sub.2 COOMe                                                                           H    (+)-pin                                        5871 OMe         CH.sub.2 COOMe                                                                           H    OH, OH                                         5872 NH(CNH)H    (CH.sub.2)CN.sub.4 H                                                                     H    OH, OH                                         5873 NH(CNH)H    (CH.sub.2)CN.sub.4 H                                                                     H    (+)-pin                                        ______________________________________                                    

                  TABLE 58                                                         ______________________________________                                          ##STR153##                                                                    Ex   X           R.sup.13  R.sup.14                                                                            Y.sup.1 Y.sup.2                                                                       Phys. Data                              ______________________________________                                         m = 1                                                                          5878 CH.sub.2 NH.sub.2                                                                          H         H    (+)-pin                                        5879 CH.sub.2 NH.sub.2                                                                          H         H    OH, OH                                         5880 NH(CNH)NH.sub.2                                                                            H         H    (+)-pin                                        5881 NH(CNH)NH.sub.2                                                                            H         H    OH, OH                                         5882 OMe         H         H    (+)-pin                                        5883 OMe         H         H    OH, OH                                         5884 NH(CNH)H    H         H    OH, OH                                         5885 NH(CNH)H    H         H    (+)-pin                                        5886 CH.sub.2 NH.sub.2                                                                          CH.sub.2 CN                                                                              H    (+)-pin                                        5887 CH.sub.2 NH.sub.2                                                                          CH.sub.2 CN                                                                              H    OH, OH                                         5888 NH(CNH)NH.sub.2                                                                            (CH.sub.2)COOH                                                                           H    (+)-pin                                        5889 NH(CNH)NH.sub.2                                                                            (CH.sub.2)COOH                                                                           H    OH, OH                                         5890 OMe         CH.sub.2 COOMe                                                                           H    (+)-pin                                        5891 OMe         CH.sub.2 COOMe                                                                           H    OH, OH                                         5892 NH(CNH)H    (CH.sub.2)CN.sub.4 H                                                                     H    OH, OH                                         5893 NH(CNH)H    (CH.sub.2)CN.sub.4 H                                                                     H    (+)-pin                                        m = 0                                                                          5894 CH.sub.2 NH.sub.2                                                                          H         H    (+)-pin                                        5895 CH.sub.2 NH.sub.2                                                                          H         H    OH, OH                                         5896 NH(CNH)NH.sub.2                                                                            H         H    (+)-pin                                        5897 NH(CNH)NH.sub.2                                                                            H         H    OH, OH                                         5898 OMe         H         H    (+)-pin                                        5899 OMe         H         H    OH, OH                                         5900 NH(CNH)H    H         H    OH, OH                                         5901 NH(CNH)H    H         H    (+)-pin                                        5902 CH.sub.2 NH.sub.2                                                                          CH.sub.2 CN                                                                              H    (+)-pin                                        5903 CH.sub.2 NH.sub.2                                                                          CH.sub.2 CN                                                                              H    OH, OH                                         5904 NH(CNH)NH.sub.2                                                                            (CH.sub.2)COOH                                                                           H    (+)-pin                                        5905 NH(CNH)NH.sub.2                                                                            (CH.sub.2)COOH                                                                           H    OH, OH                                         5906 OMe         CH.sub.2 COOMe                                                                           H    (+)-pin                                        5907 OMe         CH.sub.2 COOMe                                                                           H    OH, OH                                         5908 NH(CNH)H    (CH.sub.2)CN.sub.4 H                                                                     H    OH, OH                                         5909 NH(CNH)H    (CH.sub.2)CN.sub.4 H                                                                     H    (+)-pin                                        ______________________________________                                    

                  TABLE 59                                                         ______________________________________                                          ##STR154##                                                                    Ex      H            U      Y.sup.1 Y.sup.2                                                                        Phys. Data                                 ______________________________________                                         m = 1                                                                          5914    CH.sub.2 NH.sub.2                                                                           S      (+)-pin                                            5915    NHC(NH)NH.sub.2                                                                             S      (+)-pin                                            5916    SC(NH)NH.sub.2                                                                              S      (+)-pin                                            5917    CH.sub.2 NH.sub.2                                                                           S      OH, OH                                             5918    NHC(NH)NH.sub.2                                                                             S      OH, OH                                             5919    SC(NH)NH.sub.2                                                                              S      OH, OH                                             5920    CH.sub.2 NH.sub.2                                                                           O      (+)-pin                                            5921    NHC(NH)NH.sub.2                                                                             O      (+)-pin                                            5922    SC(NH)NH.sub.2                                                                              O      (+)-pin                                            5923    CH.sub.2 NH.sub.2                                                                           O      OH, OH                                             5924    NHC(NH)NH.sub.2                                                                             O      OH, OH                                             5925    SC(NH)NH.sub.2                                                                              O      OH, OH                                             m = 2                                                                          5926    CH.sub.2 NH.sub.2                                                                           S      (+)-pin CA                                         5927    NHC(NH)NH.sub.2                                                                             S      (+)-pin                                            5928    SC(NH)NH.sub.2                                                                              S      (+)-pin                                            5929    CH.sub.2 NH.sub.2                                                                           S      OH, OH                                             5930    NHC(NH)NH.sub.2                                                                             S      OH, OH                                             5931    SC(NH)NH.sub.2                                                                              S      OH, OH                                             5932    CH.sub.2 NH.sub.2                                                                           O      (+)-pin                                            5933    NHC(NH)NH.sub.2                                                                             O      (+)-pin                                            5934    SC(NH)NH.sub.2                                                                              O      (+)-pin                                            5935    CH.sub.2 NH.sub.2                                                                           O      OH, OH                                             5936    NHC(NH)NH.sub.2                                                                             O      OH, OH                                             5937    SC(NH)NH.sub.2                                                                              O      OH, OH                                             ______________________________________                                          CA: HRMS Calc.: 543.2635, Found: 543.2643                                

                  TABLE 60                                                         ______________________________________                                          ##STR155##                                                                    Ex      H            U      Y.sup.1 Y.sup.2                                                                        Phys. Data                                 ______________________________________                                         m = 1                                                                          5942    CH.sub.2 NH.sub.2                                                                           S      (+)-pin                                            5943    NHC(NH)NH.sub.2                                                                             S      (+)-pin                                            5944    SC(NH)NH.sub.2                                                                              S      (+)-pin                                            5945    CH.sub.2 NH.sub.2                                                                           S      OH, OH                                             5946    NHC(NH)NH.sub.2                                                                             S      OH, OH                                             5947    SC(NH)NH.sub.2                                                                              S      OH, OH                                             5948    CH.sub.2 NH.sub.2                                                                           O      (+)-pin                                            5949    NHC(NH)NH.sub.2                                                                             O      (+)-pin                                            5950    SC(NH)NH.sub.2                                                                              O      (+)-pin                                            5951    CH.sub.2 NH.sub.2                                                                           O      OH, OH                                             5952    NHC(NH)NH.sub.2                                                                             O      OH, OH                                             5953    SC(NH)NH.sub.2                                                                              O      OH, OH                                             m = 2                                                                          5954    CH.sub.2 NH.sub.2                                                                           S      (+)-pin                                            5955    NHC(NH)NH.sub.2                                                                             S      (+)-pin                                            5956    SC(NH)NH.sub.2                                                                              S      (+)-pin                                            5957    CH.sub.2 NH.sub.2                                                                           S      OH, OH                                             5958    NHC(NH)NH.sub.2                                                                             S      OH, OH                                             5959    SC(NH)NH.sub.2                                                                              S      OH, OH                                             5960    CH.sub.2 NH.sub.2                                                                           O      (+)-pin                                            5961    NHC(NH)NH.sub.2                                                                             O      (+)-pin                                            5962    SC(NH)NH.sub.2                                                                              O      (+)-pin                                            5963    CH.sub.2 NH.sub.2                                                                           O      OH, OH                                             5964    NHC(NH)NH.sub.2                                                                             O      OH, OH                                             5965    SC(NH)NH.sub.2                                                                              O      OH, OH                                             ______________________________________                                    

                  TABLE 61                                                         ______________________________________                                          ##STR156##                                                                                                                Phys                               Ex   X          R.sup.A                                                                              R.sup.C  R.sup.D                                                                              Y.sup.1, Y.sup.2                                                                      Data                               ______________________________________                                         5970 NHC(NH)NH.sub.2                                                                           Me    Ph       OMe   (+)-pin                                   5971 NHC(NH)NH.sub.2                                                                           Me    Ph       CONH.sub.2                                                                           (+)-pin                                   5972 NHC(NH)NH.sub.2                                                                           Me    Ph       F     (+)-pin                                   5973 NHC(NH)NH.sub.2                                                                           Me    Ph       CF.sub.3                                                                             (+)-pin                                   5974 NHC(NH)NH.sub.2                                                                           Me    Ph       Cl    (+)-pin                                   5975 NHC(NH)NH.sub.2                                                                           Me    Ph       OH    (+)-pin                                   5976 NHC(NH)NH.sub.2                                                                           Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OMe   (+)-pin                                   5977 NHC(NH)NH.sub.2                                                                           Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            CONH.sub.2                                                                           (+)-pin                                   5978 NHC(NH)NH.sub.2                                                                           Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            F     (+)-pin                                   5979 NHC(NH)NH.sub.2                                                                           Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            CF.sub.3                                                                             (+)-pin                                   5980 NHC(NH)NH.sub.2                                                                           Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            Cl    (+)-pin                                   5981 NHC(NH)NH.sub.2                                                                           Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OH    (+)-pin                                   5982 SC(NH)NH.sub.2                                                                            Me    Ph       OMe   (+)-pin                                   5983 SC(NH)NH.sub.2                                                                            Me    Ph       CONH.sub.2                                                                           (+)-pin                                   5984 SC(NH)NH.sub.2                                                                            Me    Ph       F     (+)-pin                                   5985 SC(NH)NH.sub.2                                                                            Me    Ph       CF.sub.3                                                                             (+)-pin                                   5986 SC(NH)NH.sub.2                                                                            Me    Ph       Cl    (+)-pin                                   5987 SC(NH)NH.sub.2                                                                            Me    Ph       OH    (+)-pin                                   5988 SC(NH)NH.sub.2                                                                            Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OMe   (+)-pin                                   5989 SC(NH)NH.sub.2                                                                            Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            CONH.sub.2                                                                           (+)-pin                                   5990 SC(NH)NH.sub.2                                                                            Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            F     (+)-pin                                   5991 SC(NH)NH.sub.2                                                                            Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            CF.sub.3                                                                             (+)-pin                                   5992 SC(NH)NH.sub.2                                                                            Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            Cl    (+)-pin                                   5993 SC(NH)NH.sub.2                                                                            Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OH    (+)-pin                                   5994 CH.sub.2 NH.sub.2                                                                         Me    Ph       OMe   (+)-pin                                   5995 CH.sub.2 NH.sub.2                                                                         Me    Ph       CONH.sub.2                                                                           (+)-pin                                   5996 CH.sub.2 NH.sub.2                                                                         Me    Ph       F     (+)-pin                                   5997 CH.sub.2 NH.sub.2                                                                         Me    Ph       CF.sub.3                                                                             (+)-pin                                   5998 CH.sub.2 NH.sub.2                                                                         Me    Ph       Cl    (+)-pin                                   5999 CH.sub.2 NH.sub.2                                                                         Me    Ph       OH    (+)-pin                                   6000 CH.sub.2 NH.sub.2                                                                         Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OMe   (+)-pin                                   6001 CH.sub.2 NH.sub.2                                                                         Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            CONH.sub.2                                                                           (+)-pin                                   6002 CH.sub.2 NH.sub.2                                                                         Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            F     (+)-pin                                   6003 CH.sub.2 NH.sub.2                                                                         Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            CF.sub.3                                                                             (+)-pin                                   6004 CH.sub.2 NH.sub.2                                                                         Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            Cl    (+)-pin                                   6005 CH.sub.2 NH.sub.2                                                                         Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OH    (+)-pin                                   6006 NHC(NH)NH.sub.2                                                                           Me    Ph       OMe   OH, OH                                    6007 NHC(NH)NH.sub.2                                                                           Me    Ph       CONH.sub.2                                                                           OH, OH                                    6008 NHC(NH)NH.sub.2                                                                           Me    Ph       F     OH, OH                                    6009 NHC(NH)NH.sub.2                                                                           Me    Ph       CF.sub.3                                                                             OH, OH                                    6010 NHC(NH)NH.sub.2                                                                           Me    Ph       Cl    OH, OH                                    6011 NHC(NH)NH.sub.2                                                                           Me    Ph       OH    OH, OH                                    6012 NHC(NH)NH.sub.2                                                                           Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OMe   OH, OH                                    6013 NHC(NH)NH.sub.2                                                                           Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            CONH.sub.2                                                                           OH, OH                                    6014 NHC(NH)NH.sub.2                                                                           Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            F     OH, OH                                    6015 NHC(NH)NH.sub.2                                                                           Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            CF.sub.3                                                                             OH, OH                                    6016 NHC(NH)NH.sub.2                                                                           Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            Cl    OH, OH                                    6017 NHC(NH)NH.sub.2                                                                           Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OH    OH, OH                                    6018 SC(NH)NH.sub.2                                                                            Me    Ph       OMe   OH, OH                                    6019 SC(NH)NH.sub.2                                                                            Me    Ph       CONH.sub.2                                                                           OH, OH                                    6020 SC(NH)NH.sub.2                                                                            Me    Ph       F     OH, OH                                    6021 SC(NH)NH.sub.2                                                                            Me    Ph       CF.sub.3                                                                             OH, OH                                    6022 SC(NH)NH.sub.2                                                                            Me    Ph       Cl    OH, OH                                    6023 SC(NH)NH.sub.2                                                                            Me    Ph       OH    OH, OH                                    6024 SC(NH)NH.sub.2                                                                            Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OMe   OH, OH                                    6025 SC(NH)NH.sub.2                                                                            Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            CONH.sub.2                                                                           OH, OH                                    6026 SC(NH)NH.sub.2                                                                            Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            F     OH, OH                                    6027 SC(NH)NH.sub.2                                                                            Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            CF.sub.3                                                                             OH, OH                                    6028 SC(NH)NH.sub.2                                                                            Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            Cl    OH, OH                                    6029 SC(NH)NH.sub.2                                                                            Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OH    OH, OH                                    6030 CH.sub.2 NH.sub.2                                                                         Me    Ph       OMe   OH, OH                                    6031 CH.sub.2 NH.sub.2                                                                         Me    Ph       CONH.sub.2                                                                           OH, OH                                    6032 CH.sub.2 NH.sub.2                                                                         Me    Ph       F     OH, OH                                    6033 CH.sub.2 NH.sub.2                                                                         Me    Ph       CF.sub.3                                                                             OH, OH                                    6034 CH.sub.2 NH.sub.2                                                                         Me    Ph       Cl    OH, OH                                    6035 CH.sub.2 NH.sub.2                                                                         Me    Ph       OH    OH, OH                                    6036 CH.sub.2 NH.sub.2                                                                         Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OMe   OH, OH                                    6037 CH.sub.2 NH.sub.2                                                                         Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            CONH.sub.2                                                                           OH, OH                                    6038 CH.sub.2 NH.sub.2                                                                         Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            F     OH, OH                                    6039 CH.sub.2 NH.sub.2                                                                         Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            CF.sub.3                                                                             OH, OH                                    6040 CH.sub.2 NH.sub.2                                                                         Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            Cl    OH, OH                                    6041 CH.sub.2 NH.sub.2                                                                         Me    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OH    OH, OH                                    ______________________________________                                    

UTILITY

The compounds of formula (I) are useful as inhibitors of trypsin-like enzymes, notably human thrombin, Factor VIIa, Factor IXa, Factor Xa, plasma kallikrein and plasmin. Because of their inhibitory action, these compounds are indicated for use in the prevention or treatment of physiological reactions catalyzed by the aforesaid enzymes such as blood coagulation and inflammation. These compounds are also useful as anticoagulants for the processing of blood for therapeutic or diagnostic purposes or for the production of blood products of fragments, since contact of blood with the surfaces commonly used for blood collection and storage causes activation of coagulation leading to thrombin formation and clot formation.

The effectiveness of compounds of the present invention as inhibitors of blood coagulation proteases was determined using purified human proteases and synthetic substrates following procedures similar to those described in Kettner et al. (1990).

For these assays, the rate of enzymatic (thrombin, Factor Xa, and Factor VIIa) hydrolysis of chromogenic substrates (S2238 (H-D-Phe-Pip-Arg-pNA), S2222, and S2288, respectively; Kabi Pharmacia, Franklin, Ohio.) was measured both in the absence and presence of compounds of the present invention. Hydrolysis of the substrate resulted in the release of pNA, which was monitored spectrophotometrically by measuring the increase in absorbance at 405 nM. A decrease in the rate of absorbance change at 405 nm in the presence of inhibitor is indicative of enzyme inhibition. The results of this assay are expressed as inhibitory constant, K_(i).

Thrombin and Xa determinations were made in 0.10M sodium phosphate buffer, pH 7.5, containing 0.20M NaCl, and 0.5% PEG 8000. VIIa determinations were made in 0.05M tris buffer, pH 7.6, containing 0.10M NaCl, 4 mM CaCl₂, and 0.1% bovine serum albumin. The Michaelis constant, K_(m), for substrate hydrolysis was determined at 5° C. using the method of Lineweaver and Burk.

Values of K_(i) were determined by allowing 0.2-0.5 nM human thrombin or human factor Xa (Enzyme Research Laboratories, South Bend, Ind.), or 50 nM human factor VIIa (BiosPacific, Emeryville, Calif.) react with the substrate (0.20 mM-1 mM) in the presence of inhibitor. Reactions were allowed to go for 30 minutes and the velocities (rate of absorbance change vs time) were measured in the time frame of 25-30 minutes. The following relationship was used to calculate K_(i) values. ##EQU1## where: v_(o) is the velocity of the control in the absence of inhibitor;

v_(s) is the velocity in the presence of inhibitor;

I is the concentration of inhibitor;

K_(i) is the dissociation constant of the enzyme: inhibitor complex;

S is the concentration of substrate;

K_(m) is the Michaelis constant.

Using the methodology described above, representative compounds of this invention were evaluated and found to exhibit a Ki of less 500 μM thereby confirming the utility of compounds of the invention as effective inhibitors of human blood coagulation proteases. The results of these assays are summarized in Table 62, where +++ indicates a K_(i) <500 nM; ++ indicates a K_(i) <50,000 nM; and + indicates a K_(i) 500,000<nM; - indicates inactive.

                  TABLE 62                                                         ______________________________________                                         K.sub.i values for inhibition of Serine                                        Proteases by compounds of the present invention.                               EXAMPLE   Thrombin     Factor Xa                                                                               Factor VIIa                                    ______________________________________                                         1         +++          ++       NT                                             2         +++          +++      +++                                            29        +++          NT       NT                                             35        +++          +++      ++                                             68        ++           ++       +++                                            129       +++          +++      NT                                             199       +++          +++      +++                                            203       +++          +++      +++                                            224       +++          +++      +++                                            227       +++          +++      ++                                             231       +++          +++      ++                                             261       +++          +++      +++                                            262       +++          +++      +++                                            263       +++          +++      +++                                            283       +++          +++      ++                                             286       +++          +++      +++                                            288       +++          NT       +++                                            298       +++          +++      +++                                            299       +++          +++      +++                                            302       +++          +++      ++                                             303       +++          ++       ++                                             304       ++           ++       ++                                             305       ++           ++       ++                                             468       ++           ++       ++                                             474       ++           ++       ++                                             887       +++          NT       NT                                             888       +++          ++       ++                                             890       +++          ++       ++                                             892       +++          ++       ++                                             898       +++          ++       ++                                             905       ++           ++       -                                              913       +++          -        ++                                             914       +++          ++       ++                                             917       +++          ++       ++                                             920       +++          NT       NT                                             921       +++          ++       ++                                             923       +++          ++       ++                                             931       +++          ++       ++                                             967       +++          ++       +++                                            969       +++          ++       ++                                             977       +++          NT       NT                                             1352      +++          ++       NT                                             1431      +++          NT       NT                                             1459      ++           ++       ++                                             1467      +++          NT       ++                                             1521      +++          NT       NT                                             1557      +++          NT       ++                                             2066      NT           NT       NT                                             2067      +++          NT       NT                                             2068      ++           ++       ++                                             2073      +++          ++       ++                                             2074      +++          ++       ++                                             2411      +++          NT       NT                                             2412      +++          ++       ++                                             2414      +++          ++       ++                                             2416      +++          ++       ++                                             2422      +++          ++       ++                                             2430      ++           ++       -                                              2439      +++          ++       ++                                             2440      +++          ++       ++                                             2443      +++          ++       ++                                             2446      +++          ++       ++                                             2447      +++          ++       ++                                             2490      +++          ++       +++                                            2491      +++          +++      ++                                             2499      +++          ++       ++                                             2533      +++          ++       -                                              2752      +++          NT       NT                                             2780      +++          ++       +++                                            2781      +++          ++       ++                                             2837      ++           NT       NT                                             3349      +++          ++       NT                                             3458      +++          -        ++                                             3465      +++          ++       ++                                             3538      +++          ++       ++                                             4064      ++           ++       ++                                             4065      ++           ++       ++                                             5426      +++          +++      NT                                             5529      +++          +++      NT                                             5551      NT           NT       NT                                             ______________________________________                                    

The final concentration of thrombin was 4 NIH units/mL. The effectiveness of compounds in prolonging clotting times is reported as K_(i) TT (nM; level of inhibitor required to prolong clotting to the time observed for 2 NIH units/mL thrombin in the absence of inhibitor) o Compounds of the present invention were found to have K_(i) TT values in the range of 100-6000 nm.

Generally, these compounds may be administered orally or parenterally to a hose to obtain an anti-thrombogenic effect. The dosage of the active compound depends on the mammalian species, body weight, age, and mode of administration as will be obvious to one skilled in the art. In the case of large mammals such as humans, the compounds may be administered alone or in combination with pharmaceutical carriers or diluents at a dose of from 0.02 to 15 mg/Kg to obtain the anti-thrombogenic effect, and may be given as a single dose or in divided doses or as a sustained release formulation.

Pharmaceutical carriers or diluents are well known and include sugars, starches and water, which may be used to make tablets, capsules, injectable solutions or the like which can serve as suitable dosage forms for administration of the compounds of this invention. Remington's Pharmaceutical Sciences, A. Osol, is a standard reference text which discloses suitable pharmaceutical carriers and dosage forms. The disclosure of this text is hereby incorporated by reference for a more complete teaching of suitable dosage forms for administration of the compounds of this invention. 

What is claimed is:
 1. A compound of formula:

    R.sup.1 --Z--CHR.sup.2 --A                                 (I)

wherein: A is -BY¹ Y² ; Y¹ and Y² are independentlya) --OH, b) --F c) --NR³ R⁴, or d) C₁ -C₈ alkoxy; Y¹ and y² are taken together to form:e) a cyclic boron ester where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which are N, S, or O, f) a cyclic boron amide where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which are N, S, or O, g) a cyclic boron amide-ester where said chain or ring contains from 2 to 20 carbon atoms and from 0-3 heteroatoms which are N, S, or O; Z isa) --(CH₂)_(m) CONR⁸ --, b) --(CH₂)_(m) CSNR⁸ --, c) --(CH₂)_(m) SO₂ NR⁸ --, d) --(CH₂)_(m) CO₂ --, e) --(CH₂)_(m) C(S)O--, or f) --(CH₂)_(m) SO₂ O--; R¹ is --(CH₂)_(p) -aryl, wherein aryl is phenyl, naphthyl or biphenyl substituted with one, two or three substituents selected from the group consisting of:halo, methylenedioxy, -R⁸, --NR⁸ COR⁹, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, --(CH₂)_(w) --OR⁸, -(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, --(CH₂)_(w) CF₃, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CHO; --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) SO₂ NH--(C₁ -C₅)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO₂ --(phenyl), --O(C═O)--(C₁ -C₅ -alkyl), ##STR157## R² is a) -(C₁ -C₁₂ alkyl)-X, b) -(C₂ -C₁₂ alkenyl)-X, or ##STR158## X is a) halogen, b) --CN, c) --NO₂, d) --CF₃, e) --S(O)_(r) R14, f) --NHR¹⁴ g) --NHS(O)_(r) R¹⁴, h) --NHC(NH)H, i) --NHC(NH)NHOH, j) --NHC(NH)NHCN, k) --NHC(NH)NHR¹⁴, l) --NHC(NH)NHCOR¹⁴, m) --C(NH)NHR¹⁴, n) --C(NH)NHCOR¹⁴, o) --C(O)NHR¹⁴, p) --C(O)NHC(O)R¹⁴, q) --C(O)OR¹⁴, r) --OR¹⁴, s) --OC(O)R¹⁴, t) --OC(O)OR¹⁴, u) --OC(O)NHR¹⁴, v) --OC(O)NHC(O)R¹⁴, w) --SC(═NH)^(NHR) ¹⁴, or x) --SC(═NH)NHC(═O)R¹⁴ ; R³ isa) hydrogen, b) C₁ -C₈ alkyl, c) -(C₁ -C₄ alkyl)-aryl, d) C₅ -C₇ cycloalkyl, or e) phenyl; R⁴ isa) hydrogen, b) C₁ -C₈ alkyl, c) --(C₁ -C₄ alkyl)-aryl, d) C₅ -C₇ cycloalkyl, e) phenyl, or f) phenylsulfonyl; R⁷ isa) phenyl, b) C₁ -C₈ -alkyl, c) C₁ -C₄ -alkoxy, d) --CF₃, or e) benzyl; R⁸ and R⁹ are independentlya) H, ##STR159## c) C₃ -C₇ cycloalkyl, d) C₁ -C₈ -alkyl, or R¹¹ isa) halo, b) --CN, c) C₁ -C₁₀ -alkyl, d) C₃ -C₈ -cycloalkyl, e) C₂ -C₁₀ -alkenyl, f) C₂ -C₁₀ -alkynyl, g) --OR⁸, h) --NO₂, i) --CF₃, j) --S(O)_(r) R⁷, k) --NR⁸ R⁹, m) --CO₂ R⁸, l) --COR⁹, n) --CONR⁸ R⁹, or o) H R¹² is H, C₁ -C₄ alkyl, phenyl, benzyl, --COR⁷, or --S(O)_(r) R⁷ ; R14 isa) --H, b) --CF₃ c) --C₁ -C₄ alkyl, d) --(CH₂)_(q) -aryl, wherein aryl is phenyl, biphenyl, naphthyl, or fluorenyl unsubstituted or substituted with one to three substituents selected from the group consisting of:halogen, --CF₃, -(C₁ -C₄ alkyl), --(CH₂)_(x) R¹⁵, --(CH₂)_(x) CO(CH₂)_(y) R¹⁵, --(CH₂)_(x) C(O)O(CH₂)_(y) R¹⁵, --(CH₂)_(x) C(O)N (CH₂)_(y) R¹⁵ ! (CH₂)_(y) R¹⁶ !, -methylenedioxy, -(C₁ -C₄ alkoxy), --(CH₂)_(x) O(CH₂)_(y) R¹⁵, --(CH₂)_(x) OCO(CH₂)_(y) R¹⁵, --(CH₂)_(x) OC(O)O(CH₂)_(y) R¹⁵, --(CH₂)_(x) OC(O)N (CH₂)_(y) R¹⁵ ! (CH₂)_(y) R¹⁶ !, --(CH₂)_(x) OC(O)N (CH₂)_(y) R¹⁵ ! CO(CH₂)_(y) R¹⁶ !, --(CH₂)_(x) S(O)_(r) (CH₂)_(y) R¹⁵, --(CH₂)_(x) S(O)_(r) (CH₂)_(y) COR¹⁵, --(CH₂)_(x) S(O)_(r) (CH₂)_(y) C(O)OR¹⁵, --(CH₂)_(x) S(O)_(r) N (CH₂)_(y) R¹⁵ ! (CH₂)_(y) R¹⁶ ! --(CH₂)_(x) N (CH₂)_(y) R¹⁵ ! (CH₂)_(y) R¹⁶ !, --(CH₂)_(x) N (CH₂)_(y) R¹⁵ ! CO(CH₂)_(y) R¹⁶ !, --(CH₂)_(x) N (CH₂)_(y) R¹⁵ ! C(O)O(CH₂)_(y) R¹⁶ !, --(CH₂)_(x) N (CH₂)_(y) R¹⁵ !CON (CH₂)_(y) R¹⁵ ! (CH₂)_(y) R¹⁶ !, --(CH₂)_(x) N (CH₂)_(y) R¹⁵ !CON (CH₂)_(y) R¹⁵ !-- CO(CH₂)_(y) R¹⁶ !, --(CH₂)_(x) N (CH₂)_(y) R¹⁵ ! S(O)_(r) (CH₂)_(y) R¹⁶ !; R¹⁵ and R¹⁶ are independentlya) hydrogen, b) C₁ -C₈ alkyl, c) -(C₁ -C₄ alkyl)-aryl, where aryl is defined above, d) C₅ -C₇ cycloalkyl, e) phenyl, substituted by 0-3 R¹⁸, f) benzyl, substituted by 0-3 R¹⁸, or g) --(C₁ -C₄ alkoxy); R¹⁵ and R¹⁶ are taken together to form a ring: ##STR160## m is 0 to 6; n is 1 to 2;p is 0 to 2; q is 0 to
 4. r is 0 to 2; s is 0 to 3; t is 1 to 5; u is 0 to 5; w is 0 to 5; x is 0 to 6; y is 0 to 6; W isa) --O--, b) --S(O)_(r), c) --NR⁴ --, d) --NC(═O)R³ --, e) a bond, or f) --(CH₂)_(n) --;or pharmaceutically acceptable salts thereof.
 2. A compound of claim 1 wherein:Z isa) --(CH₂)_(m) CONR⁸ --, b) --(CH₂)_(m) CSNR⁸ --, c) --(CH₂)_(m) SO₂ NR⁸ --, R¹ is --(CH₂)_(p) -aryl, wherein aryl is phenyl, naphthyl or biphenyl substituted with one, two or three substituents selected from the group consisting of:halo, methylenedioxy, -R⁸, --NR⁸ COR⁹, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, --(CH₂)_(w) --OR⁸, --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, --(CH₂)_(w) CF₃, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹. --(CH₂)_(w) SO₂ NH--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)--alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -perfluoroalkyl), or --(CH₂)_(w) NH--CO₂ --(phenyl), --O(C═O--(C₁ -C₅ alkyl); R¹⁴ is:a) --H, b) --CF₃ c) -C₁ -C₄ alkyl, d) --(CH₂)_(q) -aryl, wherein aryl is phenyl, biphenyl, naphthyl, or fluorenyl unsubstituted or substituted with one to three substituents selected from the group consisting of:halogen --CF₃,-(C₁ -C₄ alkyl), -methylenedioxy, -(C₁ -C₄ alkoxy), --(CH₂)_(x) N (CH₂)_(y) R¹⁵ ! (CH₂)_(y) R¹⁶ !; and all other required substituents of formula (I) are as defined in claim
 1. 3. A compound of claim 2 whereinA is -BY¹ Y² ; Y¹ and Y² are independentlya) --OH, or b) C₁ -C₈ alkoxy; Y¹ and Y² are taken together to forma cyclic boron ester where said chain or ring contains from 2 to 20 carbon atoms and from 0-3 heteroatoms which are N, S, or O, X isa) halogen b) --CN, c) --NO₂, d) --CF₃, e) --NHR¹⁴ f) --NHS(O)_(r) R¹⁴, g) --NHC(NH)H, h) --NHC(NH)NHOH, i) --NHC(NH)NHCN, j) --NHC(NH)NHR¹⁴, k) --NHC(NH)NHCOR¹⁴, l) --C(NH)NHR¹⁴, m) --C(NH)NHCOR¹⁴, n) --C(O)NHR¹⁴, o) --C(O)NHC(O) R¹⁴, p) --C(O)OR¹⁴, q) --OR¹⁴, r) --OC(O)R¹⁴, s) --OC(O)OR¹⁴, t) --OC(O)NHR¹⁴, u) --OC(O)NHC(O) R¹⁴, v) --SC(═NH)NHR¹⁴, or w) --SC(═NH)NHC(═O) R¹⁴ ; W isa) --O--, b) --NR⁴ --, c) a bond, or d) --(CH₂)_(n) --;and all other required substituents of formula (I) are as in claim
 2. 4. A compound of claim 3 wherein:Z is --(CH₂)_(m) CONR⁸ --; R² isa) -(C1-C12 alkyl)-X, or ##STR161## X is a) halogen (F, Cl, Br, I), b) --CN, c) --NHR¹⁴ d) --NHC(NH) H, e) --NHC(NH) NHR¹⁴, f) --C(NH)NHR¹⁴, g) --OR¹⁴, or h) --SC(═NH) NHR¹⁴ ; R¹⁴ is --H;and all other required substituents of formula (I) are defined as in claim
 3. 5. A compound of claim 4 selected from the group consisting of:N¹ -(4-phenylbenzoyl)-(R)-boroarginine, hydrochloride N¹ -(3-phenoxybenzoyl)-(R)-boroarginine, hydrochloride N¹ -(1-fluorenonyl)-(R)-boroarginine, hydrochloride N¹ -(4- 1-butyl!benzoyl)-(R)-boroarginine, hydrochloride N¹ -(2-benzoylbenzoyl)-(R)-boroarginine, hydrochloride N¹ -(3- N-benzyloxycarbonyl-N-methylamino!-4- 1-butyl!-benzoyl)-(R)-boroarginine, hydrochloride N¹ -(4-cyclohexylbenzoyl)-(R)-boroarginine, hydrochloride N¹ -(2-methyl-4-phenylbenzoyl)-(R)-boroarginine, hydrochloride N¹ - 4-phenyl-2-nitrobenzoyl!boroArg, (+)-pinanediol ester N¹ - 4-phenyl-2-fluorobenzoyl!boroArg, (+)-pinanediol ester N¹ - 4-phenyl-2-aminobenzoyl!boroArg, (+)-pinanediol ester N¹ - 4-phenyl-2-(methylsulfonamido)benzoyl!boroArg, (+)-pinanediol ester N¹ - 4-phenyl-2-(cyanomethylamino)benzoyl!boroArg, (+)-pinanediol ester N¹ - 4-phenyl-2-(cyanomethyl)benzoyl!boroArg, (+)-pinanediol ester N¹ - 4-phenyl-2-(diethylamino)benzoyl!boroArg, (+)-pinanediol ester N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)pinanediol ester N¹ - 4- 2-(aminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)pinanediol ester N¹ - 4- 2-(methoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)-pinanediol ester N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!benzoyl!boroArg, (+)-pinanediol ester N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!benzoyl!boroArg--OH N¹ - 4- 2-(n-butoxycarbonylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)-pinanediol ester N¹ - 4- 2-(diethylaminosulfonyl)phenyl!-2-methyl-benzoyl!boroArg, (+)pinanediol ester N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg, (+)pinanediol ester N¹ - 4- 2-(aminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg, (+)pinanediol ester N¹ - 4- 2-(methoxycarbonylaminosulfonyl)phenyl!-2-fluoro-benzoyl!boroArg, (+)-pinanediol ester N¹ - 4- 2-(t-butylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg, (+)pinanediol ester N¹ - 4- 2-(aminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg, (+)pinanediol ester N¹ - 4- 2-(methoxycarbonylaminosulfonyl)phenyl!-2-nitro-benzoyl!boroArg, (+)-pinanediol ester N¹ -(3-phenylbenzoyl)boroarg, (+)-pinanediol N¹ - 4-(3-BOCNHphenyl)₂ -methylbenzoyl!boroarg, (+)-pinanediol N¹ - 4-(3-nitrophenyl)benzoyl!boroarg, (+)-pinanediol N¹ - 4-(3-aminophenyl)benzoyl!boroarg, (+)-pinanediol N¹ -(3-phenylbenzoyl)borolys, (+)-pinanediol and N¹ -(3-phenylbenzoyl)boroIrg, (+)-pinanediol.
 6. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of any one of claims 1 through
 5. 7. A method of treating a physiological disorder in a warm blooded animal catalyzed by trypsin-like enzymes comprising administering to an animal in need of such treatment an effective amount of a compound of any one of claims 1 through
 5. 